cas 3959-23-7, (PHENYLSULPHONYL)ACETIC ACID

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Discovery of β-carboline-(phenylsulfonyl)furoxan hybrids as potential anti-breast cancer agents
The cytotoxicity properties of the β-carboline alkaloids have been broadly investigated. However, the potential application of β-carbolines was hindered due to the moderate activity in cancer. In the present study, thirty β-carboline-(phenylsulfonyl)furoxan hybrids (11a–j, 12a–j and 13a–j) were designed and synthesized through esterification and amidation reaction strategy, and their inhibitory activities against the human breast cancer cell lines MCF-7 and MDA-MB-231 were evaluated by CCK-8 assay. Biological evaluation presented that the most promising amide derivative 13h, substituted with p-methoxyphenyl group at position 1, generated high concentration of NO and evidently depressed the MCF-7 (IC50 = 0.89 μM) and MDA-MB-231 (IC50 = 0.62 μM) cells proliferation. Particularly, the wound healing and transwell assays demonstrated that 13h significantly inhibited the migration and invasion of MDA-MB-231cells. Furthermore, the preliminary mechanisms studies indicated that 13h induced G2/M phase arrest and apoptosis possibly causing by ROS accumulation and ROS-mediated DNA damage. Based on these considerations, 13h may be a promising antimetastatic agent for breast cancer, which is noteworthy for further exploration.
Hu, Xu,Gao, Xiang,Gao, Gang,Wang, Yanbing,Cao, Hao,Li, Dahong,Hua, Huiming
(2021/04/02)

Chromone 3-position nitric oxide donor derivative as well as preparation method and application thereof
The invention relates to the fields of natural medicines and medicinal chemistry, and relates to a preparation method of a series of chromone 3-position nitric oxide donor derivatives with antitumor activity and a new application of the chromone 3-position nitric oxide donor derivatives in preparation of antitumor medicines. The chromone 3-position nitric oxide donor derivative and the pharmaceutically acceptable salt thereof are shown as a general formula I in the specification. Wherein R and R1 are described in the claims and the specification.
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(2021/05/05)

Chromone 3-piperazine linked furazan derivative as well as preparation method and application thereof
The invention relates to the fields of natural medicines and medicinal chemistry, and relates to a preparation method of a series of chromone 3-piperazine linked furazan derivatives with antitumor activity and a new application of the chromone 3-piperazine linked furazan derivatives in preparation of antitumor medicines. The chromone 3-piperazine linked furazan derivative and the pharmaceutically acceptable salt thereof disclosed by the invention are as shown in a general formula I in the specification. Wherein R is described in the claims and the specification.
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(2021/05/05)

Chromone 2-position nitric oxide donor derivative as well as preparation method and application thereof
The invention relates to the fields of natural medicines and medicinal chemistry, and relates to a preparation method of a series of chromone 2-position nitric oxide donor derivatives with antitumor activity and a new application of the chromone 2-position nitric oxide donor derivatives in preparation of antitumor medicines. The chromone 2-position nitric oxide donor derivative and the pharmaceutically acceptable salt thereof are shown as a general formula I in the specification. Wherein R and R1 are described in the claims and the specification.
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(2021/05/05)

Chromone 2-piperazine linked furazan derivative as well as preparation method and application thereof
The invention relates to the fields of natural medicines and medicinal chemistry, and relates to a preparation method of a series of chromone 2-piperazine linked furazan derivatives with antitumor activity and a new application of the chromone 2-piperazine linked furazan derivatives in preparation of antitumor medicines. The chromone 2-piperazine linked furazan derivative and the pharmaceutically acceptable salt thereof disclosed by the invention are as shown in a general formula I in the specification. Wherein R is described in the claims and the specification.
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(2021/05/05)

Evaluation of novel paclitaxel-loaded NO-donating polymeric micelles for an improved therapy for gastroenteric tumor
This study reports the design and synthesis of NO-donating polymer to generate biodegradable polymeric micelle containing paclitaxel (NO/PTX) as a nanomedicine delivery system aimed to enhance the solubility and anti-cancer activity of paclitaxel (PTX). NO/PTX showed greater NO-releasing performance than nitroglycerin, displaying excellent tolerance in KM mice, and exhibited a two-fold stronger antiproliferative activity than PTXin vitroagainst HCT116, SW480, and SGC-7901 cell lines.In vivotumor growth inhibition assay results indicated that NO/PTX displayed lightly stronger activities against tumor growth than PTX at a dose of 10 mg kg?1, while the anti-tumor effect of NO/PTX was significantly improved than that of PTX and Genexol-PM groups at a dose of 15 mg kg?1(the inhibition rate: 67%vs.53% and 41%). In addition, NO/PTX showed an improved area under the plasma concentration-time curve and drug deposition in tumors in comparison to PTX. Wound healing assay and western blot analysis of EMT-related markers suggested that NO/PTX could inhibit the potential of HCT116 migration. Western blot analysis also demonstrated that NO/PTX dampened efflux activity of P-gp and up-regulated apoptosis-related proteins. Overall, these promising results suggested that the synergism between PTX and NO-donating micelles could contribute to the potent anti-cancer activity of NO/PTX.
Fang, Yuanying,Jin, Yi,Li, Huilan,Li, Xiang,Liu, Ronghua,Tu, Liangxing,Xu, Guoliang,Yang, Zunhua
p. 13763 - 13774
(2021/08/16)

COMPOSITES, METHODS AND USES THEREOF
The present invention relates, in general terms, to methods of catalysing a reaction, including the steps of contacting a chemical entity comprising a sulphide moiety with a composite and an oxidant. The composite acts as a heterogeneous catalyst to oxidise the sulphide moiety. The present invention also relates to composites, methods of synthesising the composites and its use as a catalyst thereof.
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(2021/06/04)

Antiproliferative chromone derivatives induce K562 cell death through endogenous and exogenous pathways
A series of furoxan derivatives of chromone were prepared. The antiproliferative activities were tested against five cancer cell lines HepG2, MCF-7, HCT-116, B16, and K562, and two normal human cell lines L-02 and PBMCs. Among them, compound 15a exhibited the most potent antiproliferative activity. It was also found 15a produced more than 8 μM of NO at the peak time of 45 min by Griess assay. Generally, antiproliferative activity is positively related to NO release to some extent. Further in-depth studies on apoptosis-related mechanisms showed that 15a caused S-phase cell cycle arrest in a concentration-dependent manner and induced apoptosis significantly through mitochondria-related pathways. Human apoptosis protein array assay also demonstrated 15a increased the expression levels of pro-apoptotic Bax, Bad, HtrA2 and Trail R2/DR5. The expression of catalase and cell cycle blocker claspin were similarly up-regulated. In balance, 15a induced K562 cells death through both endogenous and exogenous pathways.
Cao, Hao,Hua, Huiming,Huang, Xiaofang,Jiao, Runwei,Li, Dahong,Li, Haonan,Li, Zhanlin,Liu, Weiwei,Xu, Fanxing,Zang, Linghe
p. 759 - 772
(2020/04/01)

Identification of New Nitric Oxide-Donating Peptides with Dual Biofilm Eradication and Antibacterial Activities for Intervention of Device-Related Infections
Implantable medical device-related infections with biofilms have become a significant challenge in clinics. Based on the potential bacteria biofilm dispersing effect of nitric oxide (NO) and the unique antibacterial activity of antimicrobial peptides (AMP), we synthesized five peptides and selected the most potent one to conjugate its N-terminal with a furoxan moiety to offer a hitherto unknown NO-donating antimicrobial peptide (FOTyr-AMP), which exhibited Staphylococcus aureus and Escherichia coli biofilm dispersion and eradication, and potent antibacterial activities in vitro. In an implanted biofilm infection mice model, topical subcutaneous injection of FOTyr-AMP allowed synergetic eradication of bacterial biofilms and potent antibacterial activity, superior to the antibiotic cephalosporin C. Given the low hemolysis effect, little influence on the blood pressure, and potent in vivo efficacy of FOTyr-AMP, it is clear that subcutaneous administration of FOTyr-AMP could be a promising approach for the intervention of medical device-related biofilm infections with desirable safety.
Fei, Yue,Wu, Jianbing,An, Hong-Wei,Zhu, Kai,Peng, Bo,Cai, Junquan,Zhang, Yihua,Li, Li-Li,Wang, Hao,Huang, Zhangjian
p. 9127 - 9135
(2020/10/18)

NO donor-type large yellow acid derivatives, their preparation method and medical use (by machine translation)
The present invention relates to the field of pharmaceutical chemistry and drug therapeutics, in particular to NO donor-type large yellow acid derivative and its preparation method and application in pharmacy. The compound has anti-tumor effect, can be used for preparing anti-tumor drug. The invention also relates to a method for preparing such compounds. (by machine translation)
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(2019/05/04)

Furoxan azoxyNO donor type tadine derivative and preparation method thereof (by machine translation)
The invention discloses a furoxan azoxyNO donor type tadine derivative and a preparation method, and belongs to the technical field of chemical synthesis of medicines: the invention has the following structural formula shown in the general formula. Wherein. In addition, coumaric acid is selected as a connecting base, so that the curative effect; in addition, the compound disclosed by the invention can effectively release NO, and beneficial attempts are made for development of NO donor anti-atherosclerotic drugs in an external mode, and the method has the advantages of effectively improving the curative effect of drugs. 4 - R1 R2 (by machine translation)
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(2019/10/01)

Design, synthesis and apoptosis-related antiproliferative activities of chelidonine derivatives
To get chelidonine derivatives with enhanced antiproliferative activity and selectivity, a series of nitric oxide donating derivatives (10a-f and 11a-j) were designed, synthesized and biologically evaluated. Compared with chelidonine, these compounds exhibited lower IC50 values against human hepatoma cells HepG2, breast cancer cells MCF-7, colon cancer cells HCT-116, as well as leukemia cells K562. Compound 11j displayed the strongest antiproliferative activity with IC50 values of 3.91, 6.90, 4.36 and 1.12 μM against the above four cells, respectively. Nevertheless, it showed an IC50 value >40 μM against human peripheral blood mononuclear cells (PBMCs), which demonstrated high selectivity between normal and cancer blood cells. In further mechanism studies, 11j showed the capability to induce K562 cells apoptosis, S phase cell cycle arrest and mitochondrial membrane potential disorder. Besides, 11j was found to be effective in promoting the expression of proapoptotic protein Bad and suppressing the expression of anti-apoptotic proteins Bcl-xL, catalase, survivin, claspin and clusterin.
Cheng, Keguang,Gao, Xiang,Hu, Xu,Hua, Huiming,Huang, Xueyan,Li, Dahong,Li, Haonan,Li, Zhanlin,Liu, Lilin,Xu, Fanxing
(2020/01/03)

Palladium-Catalyzed [3 + 2]-C-C/N-C Bond-Forming Annulation
The synthesis of bi- and tricyclic structures incorporating pyrrolidone rings is disclosed, starting from resonance-stabilized acetamides and cyclic α,β-unsaturated-γ-oxycarbonyl derivatives. This process involves an intermolecular Tsuji-Trost allylation/intramolecular nitrogen 1,4-addition sequence. Crucial for the success of this bis-nucleophile/bis-electrophile [3 + 2] annulation is its well-defined step chronology in combination with the total chemoselectivity of the former step. When the newly formed annulation product carries a properly located o-haloaryl moiety at the nitrogen substituent, a further intramolecular keto α-arylation can join the cascade, thereby forming two new cycles and three new bonds in the same synthetic operation.
Liu, Yang,Mao, Zhongyi,Pradal, Alexandre,Huang, Pei-Qiang,Oble, Julie,Poli, Giovanni
supporting information
p. 4057 - 4061
(2018/07/15)

Design and synthesis of novel senkyunolide analogues as neuroprotective agents
A class of senkyunolide analogues bearing benzofuranone fragment were designed, synthesized and evaluated for their neuroprotective effect in models of oxygen glucose deprivation (OGD) and oxidative stress. All tested compounds showed neuroprotection profile based on the cell viability assay. In particular, derivatives 1f–1i possessing furoxan-based nitric oxide releasing functionality exhibited significant biological activities in OGD models. More importantly, compound 1g containing short linker with furoxan displayed the most potent neuroprotection at the concentration of 100 μM (cell survival up to 145.2%). Besides, 1g also showed the middle level neuroprotective effect in model of oxidative stress.
Fang, Yuanying,Wang, Rikang,Wang, Qi,Sun, Yongbing,Xie, Saisai,Yang, Zunhua,Li, Min,Jin, Yi,Yang, Shilin
p. 668 - 672
(2018/01/27)

Design, synthesis and biological evaluation of novel furoxan-based coumarin derivatives as antitumor agents
In order to find new anticancer drugs, a series of novel furoxan-based coumarin derivatives (10a–k) were synthesized and evaluated for their antiproliferative activities in vitro. All compounds displayed more potent inhibition on human cervical cancer HeLa cell proliferation than coumarin-3-carboxylic acid, and compounds 10b, 10c, 10f, 10h, and 10i with IC50 values ranging from 0.88 to 5.95 μM were even stronger than doxorubicin (IC50 = 10.21 μM). The further study showed that compound 10i exerted the highest antiproliferative activity (IC50 = 0.60 μM) against human breast cancer MCF-7 cells, and compound 10f had broader spectrum antiproliferative activity against five cancer cells with IC50 values in the low micromolar range of 1.86–9.85 μM. More interestingly, compound 10f had little effect on normal intestinal epithelial CCD841 cells. Our findings suggest that these novel furoxan-based coumarin derivatives may provide a new framework for the discovery of novel antitumor agents for the intervention of human carcinoma cells.
Zhang, Zhuo,Bai, Zhi-Wei,Ling, Yong,He, Li-Qin,Huang, Peng,Gu, Hong-Xia,Hu, Rong-Feng
p. 1198 - 1205
(2018/03/26)

Discovery of novel NO-releasing celastrol derivatives with Hsp90 inhibition and cytotoxic activities
To develop multifunctional drugs, a series of celastrol/NO donor hybrids were designed, synthesized and evaluated. The detection of NO release amounts showed that the more NO of these hybrids released, the more tumor cells were inhibited. 11b, which released the highest level of NO in vitro, exhibited superior potency (IC50 = 0.48 ± 0.06 μM) compared to the other compounds. Further pharmacological studies showed that 11b induced dysregulations of the Hsp90 clients (Akt and Cdk4), apoptosis, and cell cycle arrested at G0/G1 phase against A549 cells. These results suggested that inhibition of Hsp90 and release of NO was synergistic in cancer cells. Overall, the NO-releasing capacity and the inhibition of Hsp90 pathway signaling might explain the potent anti-proliferative activities of these compounds.
Li, Na,Xu, Manyi,Bao, Na,Shi, Wei,Li, Qixing,Zhang, Xiaowei,Sun, Jianbo,Chen, Li
p. 1 - 8
(2018/10/20)

Quinoline quinine derivative as well as preparation method and application
The invention discloses a quinoline quinine derivative or pharmaceutically acceptable salt, which is of a structure shown in a general formula Ia or Ib shown in the specification. By combination of structural characteristics, structure-function relationships and pharmacophore characteristics of quinoline quinine and furazan nitric acid, on the basis of a quinoline quinine structure, a furazan nitric acid NO donor is introduced; alcohol amines with different lengths are used as connection chains, so that a novel quinoline quinine derivative with NQO1 inhibition activity is designed and synthesized. Research results show that the compound disclosed by the invention has a strong inhibition effect on proliferation of various cells, and can obviously induce ROS expression of tumor cells to synergistically promote apoptosis or necrosis of the tumors.
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(2020/09/20)

Influence of sulfur groups on carboxylic acid strengths
The relative acid strength for a series of monocarboxylic acids of the general formula R–X–(CH2)n–COOH and related dicarboxylic acids of the general formula HOOC–(CH2)n–X–(CH2)n–COOH, where R = Ph or Me, X = CH2, –S– –SO– or –SO2–; and n = 1 or 2 as appropriate; have been studied as a function of X. It is found that sulfur containing acids have lower pKa values than the corresponding carbon analogues, that the pKa is highest for the thioacids and lowest for the sulfonyl acids, that the pKas increase as n increases, and that for the dicarboxylic acid systems only the thio members show a significant reduction in pKa (2) – pKa (1) differences upon changing n from 1 to 2.
Boschmann, Erwin,Miller, Roger D.
p. 2617 - 2619
(2018/04/30)

Nitric oxide-donating derivatives of hederacolchiside A1: Synthesis and biological evaluation in vitro and in vivo as potential anticancer agents
A series of nitric oxide (NO) donating derivatives of hederacolchiside A1bearing triterpenoid saponin motif were designed, synthesized and evaluated for their anticancer activity. All of the tested furoxan-based NO releasing compounds showed significant proliferation inhibitory activities. Especially compound 6a exhibited strong cytotoxicity (IC50= 1.6–6.5 μM) against four human tumor cell lines (SMMC-7721, NCI-H460, U251, HCT-116) in vitro and the highest level of NO releasing. Furthermore, compound 6a was revealed low acute toxicity to mice and weak haemolytic activity with potent tumor growth inhibition against mice H22 hepatocellular cells in vivo (51.5%).
Fang, Yuanying,Wang, Rikang,He, Mingzhen,Huang, Hesong,Wang, Qi,Yang, Zunhua,Li, Yan,Yang, Shilin,Jin, Yi
p. 98 - 101
(2016/12/14)

Nitric oxide-releasing derivatives of brefeldin A as potent and highly selective anticancer agents
A series of NO-donating mono- or diester derivatives of brefeldin A were designed, synthesized and biologically evaluated. Some derivatives exhibited potent antiproliferative activity with low IC50 values. The most potent NO-donating hybrid 13b exhibited stronger cytotoxicity against human prostate cancer PC-3?cells, human colon carcinoma HT-29?cells and human liver cancer HepG-2?cells than BFA with IC50 values of 25?nM, 160?nM and 180?nM, respectively. More importantly, compound 13b showed good selectivity between human normal and tumor liver cells with selectivity index of 33. Additionally, 13b released higher levels of NO in HepG-2?cells than L-02?cells. Further mechanism concerning cellular apoptosis showed that 13b induced apoptosis and S phase cell cycle arrest in HepG-2?cells. Incubation with 13b increased the number of HepG-2?cells with collapsed mitochondrial membrane at low concentrations in dose-dependent manner. In addition, by using the Human Apoptosis Protein Array kit, several apoptosis-related proteins, including HO-1, HO-2 and survivin, were found to be markedly downregulated by 13b in HepG-2?cells. Furthermore, in western blot assay, 13b increased the expression of Bax, Cyt c and caspase 3, and reduced the relative levels of Bcl-2, Bcl-xl and pro-caspase 3 in HepG-2?cells.
Tian, Kangtao,Xu, Fanxing,Gao, Xiang,Han, Tong,Li, Jia,Pan, Huaqi,Zang, Linghe,Li, Dahong,Li, Zhanlin,Uchita, Takahiro,Gao, Ming,Hua, Huiming
p. 131 - 143
(2017/05/10)

Novel NO-releasing plumbagin derivatives: Design, synthesis and evaluation of antiproliferative activity
A series of plumbagin/NO donor hybrids were designed, synthesized and evaluated in vitro against triple negative breast cancer (MDA-MB-231), hepatocellular (HepG2) and lung (A549) carcinoma cells. Most furoxan-based plumbagin derivatives exhibited significantly superior potency compared to their parent compound. Noticeably, MDA-MB-231 cells are the most sensitive to these furoxan-based plumbagin derivatives as evidenced by IC50 values ranging from 1.24 to 5.20 μM. Besides, NO released amounts detection of all hybrids suggested that in most cases, the antiproliferative activities were positively correlated with the levels of intracellular NO release in MDA-MB-231 cells. The most active compound (11a) also possessed higher chemical stability at different pHs (6.0, 7.4 and 8.0) than plumbagin. Together, the above promising results warrant the future potential of plumbagin/NO hybrids as the lead compounds against triple negative breast cancer deserving further research.
Bao, Na,Ou, Jinfeng,Xu, Manyi,Guan, Fuqin,Shi, Wei,Sun, Jianbo,Chen, Li
p. 88 - 95
(2017/05/31)

Discovery of novel antitumor nitric oxide-donating β-elemene hybrids through inhibiting the PI3K/Akt pathway
A series of novel furoxan-based NO-donating β-elemene hybrids were designed and synthesized to improve the anticancer efficacy of natural β-elemene. The bioassay results indicated that all of the target compounds exhibited significantly improved antiproliferative activities against three cancer cell lines (SGC-7901, HeLa and U87) compared to parent compound β-elemene. Interestingly, these compounds displayed excellent sensitivity to U87?cells with IC50 values ranging from 173 to 2?nM. Moreover, most compounds produced high levels of NO in?vitro, and the antitumor activity of 11a in U87?cells was markedly attenuated by an NO scavenger (hemoglobin or carboxy-PTIO). Further mechanism studies revealed that 11a caused the G2 phase arrest of the cell cycle and induced apoptosis of U87?cells by preventing the activation of the PI3K/Akt pathway. Moreover, 11a significantly suppressed the tumor growth in H22 liver cancer xenograft mouse model with a tumor inhibitory ratio (TIR) of 64.8%, which was superior to that of β-elemene (TIR, 49.6%) at the same dose of 60?mg/kg. Together, the remarkable biological profiles of these novel NO-donating β-elemene derivatives may make them promising candidates for the intervention of human cancers.
Chen, Jichao,Wang, Tianyu,Xu, Shengtao,Zhang, Pengfei,Lin, Aijun,Wu, Liang,Yao, Hequan,Xie, Weijia,Zhu, Zheying,Xu, Jinyi
p. 414 - 423
(2017/05/04)

Scutellarin derivatives as apoptosis inducers: Design, synthesis and biological evaluation
To explore novel antitumor agents with high efficiency and low toxicity, a series of NO-donating scutellarin derivatives (14–17) were synthesized and the antiproliferative activities against MCF-7, HCT-116, PC-3 and HepG2 cancer cell lines were assessed. Among them, compound 14b was the strongest with IC50 values of 2.96?μM, 7.25?μM, 0.09?μM and 0.50?μM, respectively, and displayed low toxicity against normal human liver L-O2 cells with an IC50 of 47.96?μM, showing good selectivity between normal and malignant liver cells. Moreover, NO releasing ability of the derivatives has been studied. Mechanism studies of the most promising compounds 14b and 15a were carried out. The results indicated that 14b and 15a could induce apoptosis, cell cycle arrest at the S phase and led to mitochondrial dysfunction in the HepG2 and PC-3?cell lines, respectively. Furthermore, Human Apoptosis Protein Array kit assay demonstrated that 14b could induce apoptosis through down-regulating the levels of procaspase-3 and inhibiting the expression of survivin, c-IAP1, HSP27, HSP60, HSP70, HO-1/HMOX1/HSP32 and HO-2/HMOX2 in HepG2 cell line. These results guaranteed compound 14b to be a drug candidate against liver cancer for further investigation.
Han, Tong,Li, Jia,Xue, Jingjing,Li, He,Xu, Fanxing,Cheng, Keguang,Li, Dahong,Li, Zhanlin,Gao, Ming,Hua, Huiming
p. 270 - 281
(2017/05/01)

Phenylsulfonylfuroxan NO-donor phenols: Synthesis and multifunctional activities evaluation
Phenylsulfonyfuroxan nitric oxide (NO)-donor phenols were designed, synthesized and evaluated. The compounds were designed through a symbiotic approach using selected phenols and phenylsulfonylfuroxan NO-donor. The antioxidant activities of the hybrid compounds T2–T6 showed to be good in vivo. Compounds T4 and T6 revealed excellent yeast α-glucosidase inhibitory activity and anti-glycosylation activity. All of the compounds exhibited strong NO releasing activity and significant anti-platelet aggregation activity. The inhibition of platelet aggregation was more than 50% at low concentration (1.5?μM) and 95% at higher concentration (15?μM and 150?μM). The vasodilatation experiment demonstrated that the six compounds under test exhibited definite vasodilation activity (pIC50 ranged from 5.698 to 6.383), especially compound T6 (pIC50 was 6.383) which was similar to sodium nitroprusside (pIC50 was 6.786). Both anticoagulant and vasodilatation effects were correlated with their NO releasing activities. These hybrid phenylsulfonyfuroxan-based NO-donor phenols offer a multifunctional prodrug design concept for the development of therapeutic or preventive agents for metabolic syndrome.
Xie, Yundong,Yang, Yaping,Li, Sen,Xu, Yanhong,Lu, Wenfang,Chen, Zizhang,Yang, Guangde,Li, Yiping,Cao, Yongxiao,Bian, Xiaoli
p. 4407 - 4413
(2017/07/22)

NO donor matrine derivatives, its preparation method and medical use
The invention relates to the field of medical chemistry and pharmacotherapeutics, and particularly relates to an NO donor type matrine derivative and a preparation method thereof and application in pharmacy. The compounds have an anti-tumor effect and can be used for preparing anti-tumor medicines. The invention also relates to a preparation method of the compounds.
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(2017/08/08)

Furazan NO-donating scutellarin derivative with anti-tumor activity, and preparation method and application thereof
The invention relates to the field of natural medicine and medicinal chemistry, in particular to a furazan NO-donating scutellarin derivative with anti-tumor activity, and a pharmaceutically acceptable salt thereof. The invention specifically relates to the furazan NO-donating substituted scutellarin derivatives with an aliphatic chain connecting arm on uronic acid base loci, and application for preparing anti-tumor drugs. The structures of the furazan NO-donating scutellarin derivative and the pharmaceutically acceptable salt thereof are shown in the following general formula I, wherein R and R1 are disclosed in claims and specifications. The formula is shown in the specification.
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(2017/07/19)

Nitric oxide donor type coumarin derivatives, preparation methods therefor and medicinal use of nitric oxide donor type coumarin derivatives
The invention relates to the fields of pharmacochemistry and pharmacotherapeutics and particularly relates to nitric oxide donor type coumarin derivatives, preparation methods therefor and an application of the nitric oxide donor type coumarin derivatives. The compounds play a role in resisting tumors and can be applied to the preparation of antitumor drugs.
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(2017/09/01)

Furazan type NO (nitric oxide) donor scutellarin derivative with anti-tumor activity and preparation method and application thereof
The invention relates to the field of natural medicines and medicine chemistry, in particular to a furazan type NO (nitric oxide) donor scutellarin derivative with anti-tumor activity and a pharmaceutically acceptable salt thereof, and in particular to a furazan type NO donor-substituted scutellarin derivative with a piperazine ringfatty chain link arm on saccharide carboxyl sites and a preparation method and application thereof in preparing anti-tumor medicines. The structures of the furazan type NO donor scutellarin derivative with anti-tumor activity and the pharmaceutically acceptable salt thereof are shown in the formula I, wherein R and n R1 are described in the right claim and instructiondescription. The formula I is shown in the descriptionattached figure.
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(2017/08/31)

Preparation method and uses of 4-site furazan NO-donating derivatives of brefeldin A
The invention relates to the field of medicinal chemistry, and relates to derivatives obtained by modification on 4-site of brefeldin A. Particularly, the invention relates to 4-site furazan NO donor substituted brefeldin A derivatives which have antineoplastic activity, and uses of the derivatives in preparing antineoplastic drugs. The brefeldin A derivatives are as shown by a general formula I or II, shown in the description, wherein m and n are respectively integers within the range of 1 to 8.
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(2017/08/30)

Brefeldin A derivatives, and preparation method and uses thereof
The invention relates to the field of medicinal chemistry, and relates to derivatives obtained by modification on 7-site of brefeldin A. Particularly, the invention relates to 7-site furazan NO donor substituted brefeldin A derivatives, and a preparation method of the derivatives and uses of the derivatives in preparing antineoplastic drugs. The brefeldin A derivatives are as shown by a general formula I or II, shown in the description, wherein m and n are respectively integers within the range of 1 to 8.
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(2017/08/30)

Antiproliferative activity and apoptosis inducing effects of nitric oxide donating derivatives of evodiamine
The first series of nitric oxide donating derivatives of evodiamine were designed and prepared. NO releasing ability of all target derivatives was evaluated in BGC-823, Bel-7402 and L-02 cells. The cytotoxicity was evaluated against three human tumor cell lines (Bel-7402, A549 and BGC-823) and normal human liver cells L-02. The nitrate derivatives 11a and 11b only exhibited moderate activity and furoxan-based derivatives 13a-c, 14a and 14b showed promising activity. 13c showed good cytotoxic selectivity between tumor and normal liver cells and was further investigated for its apoptotic properties on human hepatocarcinoma Bel-7402 cells. The molecular mode of action revealed that 13c caused cell-cycle arrest at S phase and induced apoptosis in Bel-7402 cells through mitochondria-related caspase-dependent pathways.
Zhao, Nan,Tian, Kang-Tao,Cheng, Ke-Guang,Han, Tong,Hu, Xu,Li, Da-Hong,Li, Zhan-Lin,Hua, Hui-Ming
p. 2971 - 2978
(2016/06/13)

Synthesis, biological activity, and apoptotic properties of NO-donor/enmein-type ent-kauranoid hybrids
Herein, we reported on a series of synthetic nitric oxide-releasing enmein-type diterpenoid hybrids (9a–i). All the target compounds showed potent antibacterial activity against selected Gram-positive bacteria S. aureus and B. subtilis. The antiproliferative activity against human tumor K562, MGC-803, CaEs-17 and Bel-7402 cells, and human normal liver cells L-02 was tested and the structure activity relationships (SARs) were also concluded. Compounds 9b and 9d showed the best activity against S. aureus and B. subtilis with the same minimal inhibitory concentrations (MICs) of 4 and 2 μg/mL, respectively. The derivative 9f displayed IC50 values of 1.68, 1.11, 3.60 and 0.72 μM against the four cancer cell lines above and 18.80 μM against normal liver cells L-02; meanwhile, 9f also released a high level of NO at the time point of 60 min of 22.24 μmol/L. Furthermore, it was also found that 9f induced apoptosis via the mitochondria-related pathway and arrested cell cycle of Bel-7402 cells at S phase. These findings might be important to explore new chemical entities for the main causes of in-hospital mortality of S. aureus infection, combined with a solid tumor.
Li, Dahong,Hu, Xu,Han, Tong,Xu, Shengtao,Zhou, Tingting,Wang, Zhenzhong,Cheng, Keguang,Li, Zhanlin,Hua, Huiming,Xiao, Wei,Xu, Jinyi
(2016/06/01)

Synthesis and biological activity of furoxan derivatives against Mycobacterium tuberculosis
Tuberculosis (TB) remains a serious health problem responsible to cause millions of deaths annually. The scenario becomes alarming when it is evaluated that the number of new drugs does not increase proportionally to the emergence of resistance to the current therapy. Furoxan derivatives, known as nitric oxide (NO) donors, have been described to exhibit antitubercular activity. Herein, a novel series of hybrid furoxan derivatives (1,2,5-oxadiazole 2-N-oxide) (compounds 4a-c, 8a-c and 14a-c) were designed, synthesized and evaluated in?vitro against Mycobacterium tuberculosis (MTB) H37Rv (ATCC 27294) and a clinical isolate MDR-TB strain. The furoxan derivatives have exhibited MIC90values ranging from 1.03 to 62?μM (H37Rv) and 7.0–50.0?μM (MDR-TB). For the most active compounds (8c, 14a, 14b and 14c) the selectivity index ranged from 3.78 to 52.74 (MRC-5?cells) and 1.25–34.78 (J774A.1?cells). In addition, it was characterized for those compounds logPo/wvalues between 2.1 and 2.9. All compounds were able to release NO at levels ranging from 0.16 to 44.23%. Among the series, the phenylsulfonyl furoxan derivatives (compounds 14a-c) were the best NO-donor with the lowest MIC90values. The most active compound (14c) was also stable at different pHs (5.0 and 7.4). In conclusion, furoxan derivatives were identified as new promising compounds useful to treat tuberculosis.
Fernandes, Guilherme Felipe dos Santos,de Souza, Paula Carolina,Marino, Leonardo Biancolino,Chegaev, Konstantin,Guglielmo, Stefano,Lazzarato, Loretta,Fruttero, Roberta,Chung, Man Chin,Pavan, Fernando Rogério,dos Santos, Jean Leandro
p. 523 - 531
(2016/08/11)

NO-releasing enmein-type diterpenoid derivatives with selective antiproliferative activity and effects on apoptosis-related proteins
: A series of nine enmein-type ent-kaurane diterpenoid and furoxan-based nitric oxide (NO) donor hybrids (10a-i) were designed and synthesized from commercially available oridonin (1). These hybrids were evaluated for their antiproliferative activity against Bel-7402, K562, MGC-803, and CaEs-17 human cancer cell lines and L-02 normal liver cells. The antiproliferative activity against tumor cells was stronger than the lead compound 1 and parent molecule 9 in most cases. Especially, compound 10f showed the strongest activity against human hepatocarcinoma Bel-7402 cell line with an IC50 of 0.81 μM and could also release 33.7 μmol/L NO at the time point of 60 min. Compounds 10a-i also showed cytotoxic selectivity between tumor and normal liver cells with IC50 ranging from 22.1 to 33.9 μM. Furthermore, the apoptotic properties on Bel-7402 cells revealed that 10f could induce S phase cell cycle arrest and apoptosis at low micromolar concentrations. The effects of 10f on apoptosis-related proteins were also investigated. The potent antiproliferative activities and mechanistic studies warrant further preclinical investigations.
Li, Dahong,Hu, Xu,Han, Tong,Liao, Jie,Xiao, Wei,Xu, Shengtao,Li, Zhanlin,Wang, Zhenzhong,Hua, Huiming,Xu, Jinyi
(2016/09/23)

Novel nitric oxide-releasing spirolactone-type diterpenoid derivatives with in vitro synergistic anticancer activity as apoptosis inducer
Herein, we reported the cytotoxicity, NO-releasing property, and apoptosis induced ability of two series of novel nitric oxide-releasing spirolactone-type diterpenoid derivatives (10a–f and 15a–f). All the title compounds were more potent than oridonin (7) and parent compound (9 or 14) against human tumor Bel-7402, K562, MGC-803 and CaEs-17 cells. SARs were concluded based on above data. Compound 15d exhibited the strongest antiproliferative activity with the IC50of 0.86, 1.74, 1.16 and 3.75?μM, respectively, and could produce high level (above 25?μM) of NO at the time point of 60?min. Further mechanism evaluation showed that 15d could induce S phase cell cycle arrest and apoptosis at low micromolar concentrations in Bel-7402 cells via mitochondria-related pathways. It was expected that the remarkable biological profile of the synthetic NO-releasing spirolactone-type diterpenoid analogs make them possible as promising candidates for the development of anticancer agents.
Li, Dahong,Han, Tong,Tian, Kangtao,Tang, Shuang,Xu, Shengtao,Hu, Xu,Wang, Lei,Li, Zhanlin,Hua, Huiming,Xu, Jinyi
p. 4191 - 4196
(2016/08/17)

With anti-tumor activity for NO [...] integrated tetradium alkali derivatives (by machine translation)
The present invention relates to natural medicine and the field of pharmaceutical chemistry, in particular to tetradium alkali 13-N bit modified derivative. This invention refers to these 13-N bit [...] NO donor substituted tetradium alkali derivative preparation method and evaluation of anti-tumor activity. The compound of the following structure: wherein R 1, R 2 to (CH 2) n or (CH 2) n1 O (CH 2) n2, n, n1, n2 to 1-8 integer. . (by machine translation)
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(2017/01/02)

Synthesis and biological evaluation of nitric oxide-releasing hybrids from gemcitabine and phenylsulfonyl furoxans as anti-tumor agents
A series of novel hybrids 10a-m were designed and synthesized by coupling phenylsulfonyl furoxans with gemcitabine through various diols or alcohol amine linkers, and their biological activities were evaluated in vitro. Most of the hybrids exhibited good to moderate anti-tumor activities, which are associated with NO release. In particular, hybrid 10e showed excellent anticancer activities which were more potent than or comparable to gemcitabine. However, inhibition of nucleoside transport only significantly decreased the inhibitory rates of gemcitabine against HepG2 cells but not 10e, and the inhibitory rates of 10e were partially reduced by pre-treatment with hemoglobin, demonstrating that the anti-tumor activity of 10e might result from the synergic effect of high levels of NO production and gemcitabine fragment. In addition, compound 10ecould apparently induce cell apoptosis by regulating apoptotic relative proteins. Therefore, our novel findings provide a proof of principle in the design of new furoxan/gemcitabine hybrids for the intervention of human cancers.
Li, Xianghua,Wang, Xuemin,Xu, Chenjun,Huang, Junkai,Wang, Chengniu,Wang, Xinyang,He, Liqin,Ling, Yong
p. 1130 - 1136
(2015/06/25)

Synthesis and antitumor evaluation of novel hybrids of phenylsulfonylfuroxan and epiandrosterone/dehydroepiandrosterone derivatives
Abstract Thirteen novel furoxan-based nitric oxide (NO) releasing hybrids (14a-e, 15a-e, 17b-d) of 16,17-pyrazo-annulated steroidal derivatives were synthesized and evaluated against the MDA-MB-231, HCC1806, SKOV-3, DU145, and HUVEC cell lines for their in vitro anti-proliferative activity. Most of the compounds displayed potent anti-proliferative effects. Among them, 17c exhibited the best activity with IC50 values of 20-1.4 nM against four cell lines (MDA-MB-231, SKOV-3, DU145, and HUVEC), and 1.03 μM against a tamoxifen resistant breast cancer cell line (HCC1806). Furthermore, five compounds (14a, 15a, 17b-d) were selected to screen for VEGF inhibitory activity. Compounds 15a, 17b,c showed obviously better activity than 2-Methoxyestradiol (2-ME) on reducing levels of VEGF secreted by MDA-MB-231 cell line. In a Capillary-like Tube Formation Assay, compounds 17b,c exhibited a significant suppression of the tubule formation in the concentration of 1.75 nM and 58 nM, respectively. The preliminary SAR showed that steroidal scaffolds with a linker in 3-position were favorable moieties to evidently increase the bioactivities of these hybrids. Overall, these results implied that 17c merited to be further investigated as a promising anti-cancer candidate.
Huang, Yaoqing,Liu, Mingming,Meng, Lanfang,Feng, Pan,Guo, Yalan,Ying, Minghua,Zhu, Xiuyan,Chen, Ying
p. 7 - 14
(2015/08/03)

Synthesis and antioxidant activity of bis unsaturated sulfones, bis pyrroles, and bis pyrazoles
The Michael acceptor 1,4-bis-(E)-2-(arylsulfonylvinyl)benzene was exploited to prepare a new series of bis heterocycles-(1,4-phenylene)bis(arylsulfonylpyrrole) and (1,4-phenylene)bis(arylsulfonyl pyrazole). All of the compounds were tested for antioxidant activity. Amongst the tested compounds, 1,4-bis-(E)-2-(arylsulfonylvinyl)benzene (5) was found to be the best potential antioxidant agent.
Lavanya,Prakash, T. Bhanu,Sravya,Padmavathi,Padmaja
p. 8815 - 8828
(2015/10/28)

Leishmanicidal activities of novel synthetic furoxan and benzofuroxan derivatives
A novel series of furoxan (1,2,5-oxadiazole 2-oxide) (compounds 3, 4a and -b, 13a and -b, and 14a to -f) and benzofuroxan (benzo[c][1,2,5]oxadiazole 1-oxide) (compounds 7 and 8a to -c) derivatives were synthesized, characterized, and evaluated for in vitro activity against promastigote and intracellular amastigote forms of Leishmania amazonensis. The furoxan derivatives exhibited the ability to generate nitric oxide at different levels (7.8% to 27.4%). The benzofuroxan derivative 8a was able to increase nitrite production in medium supernatant from murine macrophages infected with L. amazonensis at 0.75 mM after 48 h. Furoxan and benzofuroxan derivatives showed remarkable leishmanicidal activity against both promastigote and intracellular amastigote forms. Compounds 8a, 14a and -b, and 14d exerted selective leishmanicidal activities superior to those of amphotericin B and pentamidine. In vitro studies at pH 5.4 reveal that compound 8a is stable until 8 h and that compound 14a behaves as a prodrug, releasing the active aldehyde 13a. These compounds have emerged as promising novel drug candidates for the treatment of leishmaniasis. Copyright
Dutra, Luiz Ant?nio,De Almeida, Letícia,Passalacqua, Thais G.,Reis, Juliana Santana,Torres, Fabio A. E.,Martinez, Isabel,Peccinini, Rosangela Gon?alves,Chin, Chung Man,Chegaev, Konstantin,Guglielmo, Stefano,Fruttero, Roberta,Graminha, Marcia A. S.,Dos Santos, Jean Leandro
p. 4837 - 4847
(2014/08/18)

Hybrids of phenylsulfonylfuroxan and coumarin as potent antitumor agents
Sixteen furoxan-based nitric oxide (NO) releasing coumarin derivatives (6a-c, 8a-g, 10a, 13a,b, 15, and 17a,b) were designed, synthesized, and evaluated against the A549, HeLa, A2780, A2780/CDDP, and HUVEC cell lines. Most derivatives displayed potent antiproliferation activities. Among them, 8b exhibited the strongest antiproliferation activity on the four sensitive cell lines mentioned above and three drug resistant tumor cell lines A2780/CDDP, MDA-MB-231/Gem, and SKOV3/CDDP with IC50 values from 14 to 53 nM and from 62 to 140 nM, respectively. Furthermore, 8b inhibited the growth of A2780 in vivo and displayed lower toxicity on nontumorigenesis T29, showing good selectivity against malignant cells in vitro. Preliminary pharmacological studies showed that 8b induces apoptosis, arrests the cell cycle at the G2/M phase in the A2780 cell line, and disrupts the phosphorylation of MEK1 and ERK1. Overall, the NO-releasing capacity and the inhibition of ERK/MAPK pathway signaling may explain the potent antineoplastic activity of these compounds.
Liu, Ming-Ming,Chen, Xiao-Yu,Huang, Yao-Qing,Feng, Pan,Guo, Ya-Lan,Yang, Gong,Chen, Ying
p. 9343 - 9356
(2015/01/09)

Design, synthesis and biological evaluation of nitro oxide donating N-hydroxycinnamamide derivatives as histone deacetylase inhibitors
Novel nitro oxide (NO)-donating N-hydroxycinnamamide derivatives 12a-j were designed and synthesized by coupling the carboxyl group of N-hydroxycinnamamides with phenylsulfonylfuroxan through various diols or alkylol amines, and their in vitro biological activities were evaluated. It was discovered that most of target compounds showed good histone deacetylases (HDACs) inhibition and anti-tumor activities, particularly for 12j, which had great HDACs inhibitory activities (IC50s=0.15-0.26 μm) and antiproliferative effects (IC50s=3.21-7.12 μm) comparable to suberoylanilide hydroxamic acid (SAHA) (IC50s=0.16-1.41 μm for HDACs, IC50s=3.15-7.45 μm for cancer cell inhibition). Furthermore, compound 12j with strong antitumor activities produced high levels of NO (up to 8.0 μm of nitrites/nitrates) in colon cancer cells, and its antiproliferative activity was nearly half-diminished by hemoglobin (10 μm), an NO scavenger. These results suggest that the strong antiproliferative activity of 12j could be attributed to the additive effects of high levels of NO production and inhibition of HDAC in the cancer cells.
Tu, Shiliang,Yuan, Hang,Hu, Jie,Zhao, Chengguang,Chai, Rui,Cao, Hongfeng
p. 1185 - 1191
(2015/02/19)

Synthesis and bioactivity of furoxan-based nitric oxide-releasing colchicine derivatives as anticancer agents
A series of novel nitric oxide-donating colchicine derivatives (9a-j) were synthesized by coupling furoxan with N-methyl colchiceinamide through an appropriate spacer arm and their cytotoxicity against four human cancer cell lines in vitro were evaluated by MTT method. It was found that many of the derivatives displayed significant activity, particularly, compound 9f showed more potent cytotoxic activities than colchicine.
Shen, Li Hong,Wang, Sheng Li,Li, Hong Yu,Lai, Yi Sheng,Liu, Li Jie
p. 3294 - 3296
(2013/04/24)

TiCl4 hiocarbonyls and oxidation of sulfides in the presence of H2O2
H2O2 in combination with TiCl4 proved to be a highly reactive reagent system for the desulfurization of thioamide and thioketone derivatives in excellent yields and short reaction times with high purity. Sulfides were also found to undergo oxidation to sulfones under similar reaction conditions. In most cases, these reactions are highly selective, simple, and clean, affording products in high yields and purity.
Bahrami, Kiumars,Khodaei, Mohammad M.,Shakibaian, Vida,Khaledian, Donya,Yousefi, Behrooz H.
experimental part
p. 155 - 163
(2012/06/01)

Switching pathways: Room-temperature neutral solvolysis and substitution of amides
Stick or twist: By introducing steric hindrance at the nitrogen atom, stable linear amides bearing an electron-withdrawing α-substituent (Z=Ar, PhSO2, P(O)(OR)2, CN, or CO2R) can be induced to undergo solvolysis and substitution reactions through an elimination-addition mechanism (see picture). Key to this process is a low barrier to rotation around the amide bond and the α-substituentZ. Copyright
Hutchby, Marc,Houlden, Chris E.,Haddow, Mairi F.,Tyler, Simon N. G.,Lloyd-Jones, Guy C.,Booker-Milburn, Kevin I.
supporting information; experimental part
p. 548 - 551
(2012/02/04)

Synthesis and biological evaluation of novel furozan-based nitric oxide-releasing derivatives of oridonin as potential anti-tumor agents
To search for novel nitric oxide (NO) releasing anti-tumor agents, a series of novel furoxan/oridonin hybrids were designed and synthesized. Firstly, the nitrate/nitrite levels in the cell lysates were tested by a Griess assay and the results showed that these furoxan-based NO-releasing derivatives could produce high levels of NO in vitro. Then the anti-proliferative activity of these hybrids against four human cancer cell lines was also determined, among which, 9h exhibited the most potential anti-tumor activity with IC50 values of 1.82 μM against K562, 1.81 μM against MGC-803 and 0.86 μM against Bel-7402, respectively. Preliminary structure-activity relationship was concluded based on the experimental data obtained. These results suggested that NO-donor/natural product hybrids may provide a promising approach for the discovery of novel anti-tumor agents.
Li, Dahong,Wang, Lei,Cai, Hao,Zhang, Yihua,Xu, Jinyi
p. 7556 - 7568
(2012/09/07)

Antitumor platinum(II) complexes containing platinum-based moieties of present platinum drugs and furoxan groups as nitric oxide donors: Synthesis, DNA interaction, and cytotoxicity
Six novel platinum(II) complexes 1-6 bearing different furoxan moieties as nitric oxide (NO) donors have been designed, synthesized, and characterized by elemental analysis and 1H NMR, IR, and ESI-MS spectroscopy. The furoxan groups were introduced to the platinum complexes to release NO, which may take synergic action with the platinum-based moieties on the tumor cells. It was found that all compounds exhibited considerable cytotoxicity against human HCT-116 and SGC-7901 cell lines via DNA binding together with NO-releasing features, especially for compound 3. This finding is in accordance with the previous reports that NO hybrids show higher cytotoxicity against colon cancer cell lines compared with their parent compounds.
Zhao, Jian,Gou, Shaohua,Sun, Yanyan,Fang, Lei,Wang, Zhimei
p. 10317 - 10324
(2013/01/15)

Stereoselective control in the Staudinger reactions involving monosubstituted ketenes with electron acceptor substituents: Experimental investigation and theoretical rationalization
The stereoselectivity of the Staudinger reactions involving monosubstituted ketenes with electron acceptor substituents was investigated experimentally by determination of the product stereochemistry and theoretically via DFT calculations. The results indicate that imines preferentially attack the less sterically hindered exo-side of the ketenes to generate zwitterionic intermediates. Subsequently, for cyclic imines, the intermediates undergo a conrotatory ring closure directly to produce β-lactams, while for linear imines, the imine moiety of the intermediates isomerizes to more stable intermediates, which further undergo a conrotatory ring closure to afford trans-β-lactams. The steric hindrance and the isomerization, rather than the torquoelectronic effect, play crucial roles in controlling the stereoselectivity in the practical Staudinger reactions involving monosubstituted ketenes with electron acceptor substituents, although the unaccessible borylketene with a powerful electron acceptor group controls the stereoselectivity torquoelectronically, in theory.
Qi, Hengzhen,Li, Xinyao,Xu, Jiaxi
p. 2702 - 2714
(2011/05/19)

Novel nitric oxide-releasing derivatives of farnesylthiosalicylic acid: Synthesis and evaluation of antihepatocellular carcinoma activity
Figure Presented. Novel furoxan-based nitric oxide (NO) releasing derivatives (8a-p) of farnesylthiosalicylic acid (FTS) were synthesized. Compound 8l displayed the strongest inhibition on the proliferation of human hepatocellular carcinoma (HCC) cells in vitro, superior to FTS, sorafenib, and furoxan moiety, selectively induced high frequency of HCC cell apoptosis, and produced high levels of NO in HCC cells but not in nontumor liver cells. Furthermore, 8l exhibited low acute toxicity to mice and significantly inhibited the growth of HCC tumors in vivo and the Ras-related signaling in the tumors. Therefore, our novel findings may provide a new framework for the design of new NO-releasing furoxan/FTS hybrids for the intervention of human HCC.
Ling, Yong,Ye, Xiaolei,Zhang, Zhenzhen,Zhang, Yihua,Lai, Yisheng,Ji, Hui,Peng, Sixun,Tian, Jide
p. 3251 - 3259
(2011/06/24)

Synthesis and bioactivity of novel nitric oxide-releasing ursolic acid derivatives
A series of furoxan-based novel nitric oxide-donating ursolic acid (UA) derivatives (7a-f) were synthesized, and their cytotoxic activities against HepG2 cells in vitro were evaluated by MTT method. It was found that 7a-d and 7f showed more potent cytotoxic activities than control 5-fluorouracil and UA.
Chen, Li,Qiu, Wen,Tang, Jia,Wang, Zhi Feng,He, Shu Ying
p. 413 - 416
(2012/01/14)