- Thiazonaphthalimide derivatives: Synthesis and interaction with DNA
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The synthesis of several thiazonaphthalimide derivatives is described. The exclusive formation of angular rather than linear isomers was unequivocally demonstrated by NMR and single crystal X-ray diffraction. Their photophysical properties and ability to bind calf-Thymus DNA with affinities in the range of 104 makes them interesting candidates to probe DNA by fluorescence.
- Botz, Alexandra,Chenavier, Yves,Pécaut, Jacques,Delangle, Pascale,Gateau, Christelle
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- Hydrogen sulfide triggered molecular agent for imaging and cancer therapy
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We developed an activatable molecular reagent, PNF, triggered by intracellular H2S in the lysosome to release the therapeutic drug amonafide, which can escape from the lysosome into the nucleus to induce autophagy of cancer cells. PNF exhibits potent inhibitory activity against cisplatin-resistant tumor cell lines.
- Ge, Chao,Di, Xiaojiao,Han, Siqi,Wang, Mengmeng,Qian, Xiaoting,Su, Zhi,Liu, Hong-Ke,Qian, Yong
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- A potent aminonaphthalimide platinum(IV) complex with effective antitumor activities in vitro and in vivo displaying dual DNA damage effects on tumor cells
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A new aminonaphthalimide platinum(IV) complex was developed by incorporating aminonaphthalimide, a DNA intercalator, into the platinum(IV) system. This complex displayed potent antitumor activities against all tested tumor cell lines in vitro and showed great potential in overcoming drug resistance of cisplatin. Moreover, it remarkably inhibited the growth of CT26 xenografts in BALB/c mice without severe side effects in vivo. Then, the compound exhibited a dual DNA damage antitumor mechanism that it could interact with DNA in tetravalent form via the naphthalimide group to cause DNA lesion, and the further liberation of platinum(II) complex after reduction would induce remarkable secondary damage to DNA. Meanwhile, it caused cell apoptosis through an intrinsic apoptosis pathway by up-regulating the expression of caspase 3 and caspase 9.
- Wang, Qingpeng,Chen, Yan,Li, Guoshuai,Zhao, Yanna,Liu, Zhifang,Zhang, Ruiyan,Liu, Min,Li, Dacheng,Han, Jun
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- Design, antiviral and cytostatic properties of isoxazolidine-containing amonafide analogues
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Abstract A novel series of 5-arylcarbamoyl- and 5-arylmethyl-2-methylisoxazolidin-3-yl-3-phosphonates have been synthesized via cycloaddition of N-methyl-C-(diethoxyphosphoryl)nitrone with N-substituted naphthalimide acrylamides and N-allylnaphthalimides. All cis- and trans-isoxazolidine phosphonates obtained herein were assessed for antiviral activity against a broad range of DNA and RNA viruses. Isoxazolidines trans-9d and trans-9f exhibited the highest activity (EC50 = 8.9 μM) toward cytomegalovirus. Compounds cis- and trans-9d as well as cis- and trans-9f were found potent against HSV and Vaccinia viruses (EC50 in the 45-58 μM range), whereas isoxazolidines 10a and 10d suppressed replication of Coxsackie B4 and Punta Toro viruses (EC50 in the 45-73 μM range). Antiproliferative evaluation of all obtained isoxazolidines revealed the promising activity of cis-9b, cis-9d, trans-9d, cis-9e, trans-9e, cis-9f and trans-9f toward tested cancer cell lines with IC50 in the 1.1-19 μM range.
- Kokosza, Kamil,Andrei, Graciela,Schols, Dominique,Snoeck, Robert,Piotrowska, Dorota G.
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- Synthesis and the biological activity of phosphonylated 1,2,3-triazolenaphthalimide conjugates
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A novel series of diethyl {4-[(5-substituted-1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)- methyl]-1H-1,2,3-triazol-1-yl}alkylphosphonates designed as analogues of amonafide was synthesized. All phosphonates were assessed for antiviral activity against a broad range of DNA and RNA viruses and several of them showed potency against varicella-zoster virus (VZV) [EC50 (50% effective concentration) = 27.6-91.5 μM]. Compound 16b exhibited the highest activity against a thymidine kinase-deficient (TK-) VZV strain (EC50 = 27.59 μM), while 16d was the most potent towards TK+ VZV (EC50 = 29.91 μM). Cytostatic properties of the compounds 14a-i-17a-i were studied on L1210, CEM, HeLa and HMEC-1 cell lines and most of them were slightly cytostatic for HeLa [IC50 (50% inhibitory concentration) = 29-130 μM] and L1210 cells [IC50 (50% inhibitory concentration) =14-142 μM].
- G?owacka, Iwona E.,Gulej, Rafa?,Grzonkowski, Piotr,Andrei, Graciela,Schols, Dominique,Snoeck, Robert,Piotrowska, Dorota G.
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- A naphthalimide-polyamine conjugate preferentially accumulates in hepatic carcinoma metastases as a lysosome-targeted antimetastatic agent
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Disseminated tumors lead to approximately 90% of cancer-associated deaths especially for hepatocellular carcinoma (HCC), indicating the imperative need of antimetastatic drugs and the ineffectiveness of current therapies. Recently polyamine derivatives have been identified as a promising prospect in dealing with metastatic tumors. Herein, a novel class of naphthalimide-polyamine conjugates 8a-8d, 13a-13c, 17 and 21 were synthesized and the mechanism was further determined. The polyamine conjugate 13b displayed remarkably elevated anti-tumor and anti-metastatic effects (76.01% and 75.02%) than the positive control amonafide (46.91% and 55.77%) at 5 mg/kg in vivo. The underlying molecular mechanism indicated that in addition to induce DNA damage by up-regulating p53 and γH2AX, 13b also targeted lysosome to modulate polyamine metabolism and function in a totally different way from that of amonafide. Furthermore, the HMGB1/p62/LC3II/LC3I and p53/SSAT/β-catenin pathways were mainly involved in the inhibition of 13b-induced HCC metastasis by targeting polyamine transporters (PTs) overexpressed in HCC. At last, 13b down-regulated the concentrations of Put, Spd and Spm by modulating polyamine metabolism key enzymes SSAT and PAO, which favored the suppression of fast growing tumor cells. Taken together, our study implies a promising strategy for naphthalimide conjugates to treat terminal cancer of HCC by targeting autophagy and tumor microenvironment with reduced toxicities and notable activities.
- Ma, Jing,Li, Linrong,Yue, Kexin,Zhang, Zhansheng,Su, Shihao,Chen, Yutong,Yu, Lu,Zhang, Pengfei,Ma, Ruijuan,Li, Yingguang,Ma, Yinxia,Jia, Huinan,Wang, Chaojie,Wang, Jiajia,Xie, Songqiang
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- Novel 2-aminothiazonaphthalimides as visible light activatable photonucleases: Effects of intercalation, heterocyclic-fused area and side chains
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A new family of 2-aminothiazonaphthalimides with different side chains as novel intercalative and visible light activatable photonucleases, was designed, synthesized and quantitatively evaluated. The order of their photocleaving abilities was parallel to that of their intercalative properties. The compound with linear heterocyclic-fused chromophore could intercalate into and photocleave DNA more efficiently than the one with angular heterocyclic-fused chromophore. B2, the most efficient compound, caused obvious DNA damage at 1 μM. Mechanism experiment showed that superoxide anion was involved.
- Li, Zhigang,Yang, Qing,Qian, Xuhong
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- Naphthalimide-polyamine conjugate as well as preparation method and application thereof
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The invention discloses a naphthalimide-polyamine conjugate, which has a structural general formula as shown in I, a novel skeleton, high efficiency, low toxicity and good inhibitory activity for tumor cells. The invention also discloses a preparation method of the conjugate. Firstly, 3-amino groups with toxic and side effects of amonafide are removed, a phenylpyrazole structure fragment is introduced to the naphthalimide parent naphthalene ring, and a naphthalimide side chain with a polyamine chain is modified, acetyltransferase in vivo is prevented from acetylating the amino groups on the naphthalene ring of amonafideand, and toxic and side effects are reduced; and further by introducing a low-toxicity phenyl pyrazole active structure fragment, the naphthalimide polyamine conjugate witha novel skeleton, high efficiency and low toxicity is synthesized; and secondly, quinazoline with low toxicity is introduced to replace hydrogen atoms of amonafide 3-amino, so that the naphthalimide polyamine conjugate with anti-tumor activity and low toxicity is obtained. The invention also discloses an application of the conjugate in preparation of antitumor drugs, and good development potentialis realized.
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- Naphthalimide conjugate based on polyamine modification, preparation method and application thereof
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The invention belongs to the technical field of medicinal chemistry, and particularly relates to a naphthalimide conjugate based on polyamine modification, a preparation method and application thereof. The naphthalimide-polyamine conjugate disclosed by the invention has good anti-tumor activity, the in-vivo and in-vitro anti-liver cancer growth and metastasis activity of the naphthalimide-polyamine conjugate is better than that of amonafide, and the anti-tumor spectrum of the naphthalimide-polyamine conjugate is wide. Different from classical amonafide, the conjugate disclosed by the invention inhibits autophagy by targeting lysosomes and regulates polyamine metabolism and functions in a tumor cell microenvironment to achieve the activity of resisting growth and metastasis of liver cancer. The complex also solves the problems of poor solubility, complicated clinical compatibility, poor patient immunity in clinical application of chemotherapeutic drugs and the like of the conventional naphthalimide analogue represented by amonafide, and the naphthalimide complex capable of regulating subcellular organelles and tumor microenvironments is found for the first time, and a new thought and a research direction are provided for treating the advanced liver cancer.
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Paragraph 0070-0074
(2021/06/02)
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- Naphthalimide indole heterocyclic compound as well as preparation method and application thereof
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The invention belongs to the technical field of medicinal chemistry, and particularly relates to a naphthalimide indole heterocyclic compound as well as a preparation method and application thereof. The naphthalimide indole heterocyclic compound has good anti-tumor activity, the in-vivo and in-vitro anti-tumor activity of the naphthalimide indole heterocyclic compound is better than that of dinafide, and the anti-tumor spectrum of the naphthalimide indole heterocyclic compound is wide. Different from classical dinafide, the compound regulates and controls subcellular organelle and cell nucleus functions to reverse drug resistance by targeting the contents of key enzyme PAO (polyamine oxidase) and three endogenous small molecules Put (putrescine), Spd (spermidine) and Spm (spermine) in a tumor polyamine microenvironment, and enhances anti-tumor immune response at the same time; and the compound has good treatment potential on advanced metastatic tumors. The complex provided by the invention also solves the problems of poor solubility, complicated clinical compatibility, poor patient immunity in clinical application of chemotherapeutic drugs and the like of naphthalimide analogues represented by dinafide in the prior art, and has good water solubility.
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- Fluorescent probe for detecting tiredness level Preparation method and application thereof
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The invention discloses a fluorescence probe for detecting the level of hypoxia, a preparation method and application thereof, and can realize specific response Na. 2 S2 O4 The fluorescence probe is used for detecting the tiredness level, and the structure is as follows. The probe comprises a nitrogen-nitrogen double bond, which can be broken down in a hypoxic environment to cause fluorescence recovery of the compound. The naphthalimide is introduced as a fluorophore, and has the characteristics of stable fluorescence and high fluorescence quantum efficiency. The fluorescent probe is simple and convenient to prepare, obvious in spectral change, good in specificity effect, small in cytotoxicity, good in imaging effect and good in specificity detection Na. 2 S2 O4 , The fluorophore precursor and the anti-tumor drug nitrogen mustard compound can be released under the hypoxic condition, the tumor cell growth can be inhibited while the hypoxia imaging is carried out, the diagnosis and treatment integrated function is achieved, and the application prospect is good.
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- Tetravalent platinum naphthalimide complex, preparation method and application thereof
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The invention belongs to the technical field of medicinal chemistry, and particularly relates to a tetravalent platinum naphthalimide complex, a preparation method and application thereof. The tetravalent platinum naphthalimide complex has good anti-tumor activity, which is better than that of cis-platinum and oxaliplatin, and the tetravalent platinum naphthalimide complex has better stability than bivalent platinum like cis-platinum, carboplatin and oxaliplatin. According to the invention, the naphthalimide modified tetravalent platinum has good targeting performance on tumor cells, high selectivity on tumor cells is improved, and different from a classic divalent platinum drug, the complex provided by the invention regulates and controls subcellular organelles and cell nucleus functionsto reverse drug resistance by targeting a tumor high polyamine microenvironment, and relieves immunosuppression of T cells around tumors at the same time. The complex provided by the invention also solves the problems of poor solubility, tedious clinical compatibility, poor patient immunity in clinical application of chemotherapeutic drugs and the like of previous bivalent platinum antitumor drugs, and has good fat solubility and water solubility.
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- PERI-XANTHENOXANTHENE BISIMIDE COMPOUND, METHOD FOR PRODUCING THE SAME, ORGANIC EL ELEMENT, AND ORGANIC THIN FILM SOLAR CELL
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PROBLEM TO BE SOLVED: To provide a novel compound that can be used as an n-type semiconductor material in an organic semiconductor product such as an organic EL element and an organic thin film solar cell. SOLUTION: The present invention provides a peri-xanthenoxanthene bisimide compound represented by the formula (R is an alkyl group, a substitutable aryl group or the like; Xa1, Xa2, Y1, Y2, Z1 and Z2 independently represent H, halogen, a substitutable aryl group, an aromatic heterocyclic group or the like). SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
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- Naphthalimide Platinum(IV) Compounds as Antitumor Agents with Dual DNA Damage Mechanism to Overcome Cisplatin Resistance
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A new series of naphthalimide platinum(IV) compounds with dual DNA damage mechanism were designed, synthesized and evaluated for antitumor activities. The platinum(IV) compounds could combine with DNA and cause DNA damage via naphthalimide fragment. Then the platinum(II) complexes released in reductive microenvironment would cause remarkable secondary DNA lesions. Some title compounds exhibit good antitumor activities and are of great potential in overcoming the drug resistance of cisplatin. Furthermore, naphthalimide platinum(IV) complexes could effectively combine with HSA by electrostatic force, which would influence the drug distribution and bioactivities in vivo. Moreover, the accumulation of the tested platinum(IV) compounds in whole cells and DNA is remarkably enhanced in comparison with cisplatin and oxaliplatin.
- Wang, Qingpeng,Li, Guoshuai,Liu, Zhifang,Tan, Xiaoxiao,Ding, Zhuang,Ma, Jing,Li, Lanjie,Li, Dacheng,Han, Jun,Wang, Bingquan
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p. 4442 - 4451
(2018/10/25)
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- Naphthalimides-polyamine conjugate comprising terminal substituent group, and preparation method and application of naphthalimides-polyamine conjugate
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The invention relates to a naphthalimides-polyamine conjugate comprising a terminal substituent group. The structure is shown in a formula I and a formula II in the description, wherein l is equal to 1 or 2, m is equal to 1 or 2, n is equal to 1 or 2, X is equal to 2, 3 or 4, R1 is H, Cl, 3-NH2 or 4-NH2, and R2 is ethyl, propyl, cyclopropyl or cyclohexyl. The field for researching and utilizing polyamine compounds can be enlarged. The invention also provides a preparation method of the naphthalimides-polyamine conjugate comprising the terminal substituent group at the same time. In addition, the invention aims at providing application of the naphthalimides-polyamine conjugate comprising the terminal substituent group in preparing antitumor drugs, antitumor drug lead compounds, polyamine channel-selectivity compounds (compounds selectively acting on the polyamine channel), DNA intercalating agents, groove combining agents, antitumor drugs and the like.
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- Chemoselective Hydrogenation of Nitroarenes Catalyzed by Molybdenum Sulphide Clusters
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Herein, we describe an atom efficient and general protocol for the chemoselective hydrogenation of nitroarenes to anilines catalyzed by well-defined diimino and diamino cubane-type Mo3S4 clusters. The novel diimino [Mo3S4Cl3(dnbpy)3]+ ([5]+) (dnbpy=4,4′-dinonyl-2,2′-dipyridyl, L1) trinuclear complex was synthesized in high yields by simple ligand substitution reactions starting from the thiourea (tu) [Mo3S4(tu)8(H2O)]Cl4?4 H2O (3) precursor. This strategy has also been successfully adapted for the isolation of the diamino [Mo3S4Cl3(dmen)3](BF4) ([6](BF4)), (dmen=N,N′-dimethylethylenediamine) salt. Applying these catalysts, high selectivity in the hydrogenation of functionalized nitroarenes has been accomplished. Over thirty anilines bearing synthetically functional groups have been synthesized in 70 to 99 % yield. Notably, the integrity of the cluster core is preserved during catalysis. Based on kinetic studies on the hydrogenation of nitrobenzene and other potential reaction intermediates, the direct reduction to aniline is the preferential route.
- Pedrajas, Elena,Sorribes, Iván,Gushchin, Artem L.,Laricheva, Yuliya A.,Junge, Kathrin,Beller, Matthias,Llusar, Rosa
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p. 1128 - 1134
(2017/03/27)
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- Cancer cell-targeted two-photon fluorescence probe for the real-time ratiometric imaging of DNA damage
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Real-time imaging of DNA damage in cancer cells could provide valuable information on the formation and development of cancer. Herein, a two-photon fluorescence probe was discovered. Through sequential ICT processes, it allows successful in vivo visualization of DNA damage in cancer cells by one/two-photon microscopic imaging or by the unaided eye and a hand-held ultraviolet lamp.
- Zhang, Hua,Wang, Kui,Xuan, Xiaopeng,Lv, Qingzhang,Nie, Yamin,Guo, Haiming
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supporting information
p. 6308 - 6311
(2016/05/19)
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- Highly selective transfer hydrogenation of functionalised nitroarenes using cobalt-based nanocatalysts
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Anilines are important feedstock for the synthesis of a variety of chemicals such as dyes, pigments, pharmaceuticals and agrochemicals. The chemoselective catalytic reduction of nitro compounds represents the most important and prevalent process for the manufacture of functionalized anilines. Consequently, the development of selective catalysts for the reduction of nitro compounds in the presence of other reducible groups is a major challenge and is crucial. In this regard, herein we show that the cobalt oxide (Co3O4-NGr@C) based nano-materials, prepared by the pyrolysis of cobalt-phenanthroline complexes on carbon constitute highly selective catalysts for the transfer hydrogenation of nitroarenes to anilines using formic acid as a hydrogen source. Applying these catalysts, a series of structurally diverse and functionalized nitroarenes have been reduced to anilines with unprecedented chemo-selectivity tolerating halides, olefins, aldehyde, ketone, ester, amide and nitrile functionalities.
- Jagadeesh, Rajenahally V.,Banerjee, Debasis,Arockiam, Percia Beatrice,Junge, Henrik,Junge, Kathrin,Pohl, Marga-Martina,Radnik, J?rg,Brückner, Angelika,Beller, Matthias
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supporting information
p. 898 - 902
(2015/03/04)
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- Isomeric naphthalimides bearing pyran units: Insight into mutual relation between structure and photochromic properties
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Two novel isomeric photochromic naphthopyrans (1 and 2) containing naphthalimide moieties were prepared and studied. In the compound 1, O-atom of pyran cycle is at C-3 position of naphthalene ring, whereas, in compound 2, O-atom of pyran cycle is at C-4 position. In the compound 2 due to para-position O-atom of pyran photochrome cycle is involved into the conjugated naphthalimide system. The variety in mutual position of pyran and naphthalimide units leads to remarkable difference in photochromic characteristics. Both compounds demonstrate the switching of the fluorescence by photoinduced conversion between the closed and open forms.
- Fedorova,Sergeeva,Panchenko,Fedorov, Yu. V.,Erko,Berthet,Delbaere
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- Synthesis, photophysical and cytotoxicity evaluations of DNA targeting agents based on 3-amino-1,8-naphthalimide derived Troeger's bases
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The synthesis and characterisation of five bis-1,8-naphthalimide containing Troeger's bases 1-5 formed from their corresponding 3-amino-1,8- naphthalimide precursors 6-10 is described. The photophysical investigations of 1-5 and 6-10 were carried out in several organic solvents as well as in water and as a function of pH using UV-Vis absorption and fluorescence spectroscopies. The DNA binding affinities of 1-5 in aqueous solution at pH 7.4 were also investigated using several UV-Vis absorption and fluorescence experiments by using calf thymus DNA (ct-DNA). These molecules exhibited significant DNA binding affinities; where large binding values (Kb) in the range of 106 M-1 were determined, even in competitive media (50 mM and 160 mM NaCl at pH 7.4). Thermal denaturation measurements also showed that 1-5 significantly stabilised the DNA helix. Using linear and circular dichroism we further demonstrated that the DNA binding interaction occurs both by intercalation and by groove binding. The Troeger's bases were further shown to be rapidly taken up into cells using confocal fluorescence spectroscopy; and cytotoxic studies in HeLa and MCF-7 cells showed that most of the Troeger's bases were effective cytotoxic agents with EC50 values of between 1.1-12 μM and that all the active compounds induced programmed cell death by apoptosis, where up to 70% cellular death was observed after 24 h of incubation for 4. This journal is the Partner Organisations 2014.
- Murphy, Samantha,Bright, Sandra A.,Poynton, Fergus E.,McCabe, Thomas,Kitchen, Jonathan A.,Veale, Emma B.,Williams, D. Clive,Gunnlaugsson, Thorfinnur
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p. 6610 - 6623
(2014/08/18)
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- Development of 1,8-naphthalimides as clathrin inhibitors
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We reported the first small molecule inhibitors of the interaction between the clathrin N-terminal domain (TD) and endocyctic accessory proteins (i.e., clathrin inhibition1). Initial screening of a ~17 000 small molecule ChemBioNet library identified 1. Screening of an existing in-house propriety library identified four substituted 1,8-napthalimides as ~80-120 μM clathrin inhibitors. Focused library development gave 3-sulfo-N-(4-aminobenzyl)- 1,8-naphthalimide, potassium salt (18, IC50 ≈ 18 μM). A second library targeting the 4-aminobenzyl moiety was developed, and four analogues displayed comparable activity (26, 27, 28, 34 with IC50 values of 22, 16, 15, and 15 μM respectively) with a further four (24, 25, 32, 33) more active than 18 with IC50 values of 10, 6.9, 12, and 10 μM, respectively. Docking studies rationalized the structure-activity relationship (SAR) with the biological data. 3-Sulfo-N-benzyl-1,8-naphthalimide, potassium salt (25) with an IC50≈ 6.9 μM, is the most potent clathrin terminal domain-amphiphysin inhibitor reported to date.
- Macgregor, Kylie A.,Robertson, Mark J.,Young, Kelly A.,Von Kleist, Lisa,Stahlschmidt, Wiebke,Whiting, Ainslie,Chau, Ngoc,Robinson, Phillip J.,Haucke, Volker,McCluskey, Adam
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p. 131 - 143
(2014/02/14)
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- Unprecedented synthesis, in vitro and in vivo anti-cancer evaluation of novel triazolonaphthalimide derivatives
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An efficient synthesis method for fusing triazole ring onto the naphthalimide core was described. The anti-cancer activities of the generated triazolonaphthalimide derivatives were evaluated with five cancer cell lines. The compounds generally displayed higher potency than amonafide. 4d,4e carrying two amino side chains showed the strongest cytotoxicities. N-oxide 5, a prodrug of 4a, was designed and synthesized. The agent was expected to be activated under the hypoxic condition in tumor tissue. Compared with 4a, 5 manifested much lower cytotoxicity both in cancer cell lines and human normal cells in the in vitro assays. However, N-oxide 5 performed potent anti-cancer activity in vivo using S-180 sarcoma bearing mice. All the results suggested that 5 was a promising anti-cancer agent.
- Li, Shasha,Zhong, Wenhe,Li, Zhongjun,Meng, Xiangbao
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p. 546 - 552
(2012/03/09)
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- A new N-imidazolyl-1,8-naphthalimide based fluorescence sensor for fluoride detection
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A chemosensor is reported with high sensitivity and selectivity for detection of fluoride anion. The recognition mechanism is attributed to a fluoride-triggered disruption of the hydrogen bond between imidazole and naphthalimide moieties, resulting in a noncoplanar geometry with low fluorescence. The Royal Society of Chemistry 2012.
- Wang, Junqi,Yang, Lingyun,Hou, Chen,Cao, Haishi
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supporting information; experimental part
p. 6271 - 6274
(2012/09/05)
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- Novel efficient anticancer agents and DNA-intercalators of 1,2,3-triazol-1,8-naphthalimides: Design, synthesis, and biological activity
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Two novel series of 3-1,2,3-triazol-1,8-naphthalimides 5a-e, 7a-e were synthesized easily by employing 'click reaction'. Their bioactivities were evaluated. Compounds 5a-e were found to be more toxic against MCF-7 cells while 7a-e were more potent against
- Li, Xiaolian,Lin, Yanjie,Yuan, Yukun,Liu, Kai,Qian, Xuhong
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experimental part
p. 2299 - 2304
(2011/04/22)
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- 3-Urea-1,8-naphthalimides are good chemosensors: A highly selective dual colorimetric and fluorescent ICT based anion sensor for fluoride
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The 1,8-naphthalimide sensor 1 was developed as a colorimetric and fluorescent sensor for anions. Being the first example of such anion sensors, where the 3-position of the naphthalimide ring is used to incorporate the anion recognition moiety, in this ca
- Duke, Rebecca M.,Gunnlaugsson, Thorfinnur
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body text
p. 1503 - 1505
(2011/05/16)
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- Synthesis of chemiluminescent biotinyl naphtho[1,8-de][1,2]diazepine-1,4- diones
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A new chemiluminescent seven numbered cyclic peri hydrazide, 6-amino-2,3-dihydronaphtho[1,8-de][1,2]diazepine-1,4-dione (AH, 4), and five of its biotin conjugates with various spacer groups are synthesized. The total framework of the chemiluminescent biot
- Krishna Murthy,Ram Reddy
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p. 2512 - 2522
(2007/10/03)
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- Isoquinolones
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Benzo[de]isoquinoline-1,3-dione of Formula or a pharmaceutically acceptable salt thereof wherein R is hydrogen or a protecting group typically used in the art for protecting alcohols and R1-R5are each independently chosen from H, Cl, Br, F, straight or branched alkyl C1-C8alkyl, C3-C8cycloalkyl, heterocycle or bridged heterocycle of 4-9 atoms containing 1-3 heteroatoms, —(CR′2)nOR6, —(CR′2)nN(R6)2, —(CR′2)nNR6COR7, —(CR′2)nNR6SO2OR7, —(CR′2)nNR6SO2N(R6)2, —(CR′2)nOSO2N(R6)2, —(CR′2)nCN, —(CR′2)n(NOR6)R7, NO2, CF3, —(CR′2)nSOmR7, —(CR′2)nSOmR7, —(CR′2)nCO2R6, —(CR′2)nCON(R6)2, Ph, and any two of R1-R5may form a substituted or unsubstituted ring of 5-7 total atoms having 0-2 heteroatoms are claimed which are selective inhibitors of bacterial DNA gyrase and DNA topoisomerase useful in antibacterial agents. Methods for their preparation and formulation as well as novel intermediates useful in the preparation of the final products are also claimed.
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