- Preparation method of halogenated benzothiazepine oxide, product prepared by preparation method and application of product
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The invention discloses a preparation method of halogenated benzothiazepine oxide as well as a product prepared by the preparation method and application of the halogenated benzothiazepine oxide, andrelates to the technical field of chemical synthesis. Th
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Paragraph 0054; 0059-0061; 0080-0091
(2020/09/09)
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- Synthesis and anticancer activities of thiosemicarbazones derivatives of thiochromanones and related scaffolds
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A series of novel thiosemicarbazone analogs (4a–t, 6a–j) were synthesized and evaluated for their cytotoxic activities. The obtained results showed that thiochromanone-based thiosemicarbazones substituted primarily at the C-8 position exhibited higher cytotoxicity than the corresponding 1,1-dioxo-thiochromanone-, benzothiazepine-, and 1,1-dioxo-benzothiazepine-based analogs. Significantly, compound 4c (8-fluoro thiochromanone thiosemicarbazone) was found to be the most active and exhibited potent cytotoxicity against the MCF-7, SK-mel-2, and DU145 cancer cell lines, with IC50 values of 0.42, 0.58, and 0.43 μM, respectively. In addition, the mechanism of compound 4c induced MCF-7 cell apoptosis was preliminarily investigated through cell cycle, Annexin V-FITC/PI staining, and ROS assays, indicating that compound 4c may exert its anticancer property through ROS-mediated apoptosis.
- Li, Guobi,Li, Jincheng,Liu, Shenggui,Pan, Rongkai,Song, Jiangli,Song, Xiumei,Su, Wenyi
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- Synthesis of Novel Pterocarpen Analogues via [3?+?2] Coupling-Elimination Cascade of α,α-Dicyanoolefins with Quinone Monoimines
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By employing triethylamine as a catalyst, [3?+?2] coupling-elimination cascade of α,α-dicyanoolefins with quinone monoimines was realized. The reactions afforded various novel pterocarpen analogues with generally moderate yields (up to 75%). In addition, a plausible reaction mechanism was proposed.
- Chen, Hui,Zhao, Sihan,Cheng, Shaobing,Dai, Xingjie,Xu, Xiaoying,Yuan, Weicheng,Zhang, Xiaomei
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p. 1672 - 1683
(2019/04/08)
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- Thiochroman-4-one thiosemicarbazide compound as well as preparation method and application thereof
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The invention relates to a thiochroman-4-one thiosemicarbazide compound, as well as a preparation method and an application thereof. The structural formula of the thiochroman-4-one thiosemicarbazide compound is shown as Formula (I), wherein n is 1 or 2, R
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Paragraph 0061; 0063; 0064; 0065
(2018/11/22)
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- Ionic liquid catalyzed synthesis of 2-(indole-3-yl)-thiochroman-4-ones and their novel antifungal activities
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2-(Indole-3-yl)-thiochroman-4-ones were synthesized via ionic liquid and tested for in vitro antifungal activity. The contribution of ionic liquid to Michael addition reaction is significant. Structures of all compounds are elucidated by 1H NMR, 13C NMR and HRMS. Most of these compounds showed better antifungal activity than fluconazole. The results suggest that 2-(indole-3-yl)-thiochroman-4-ones would be efficient antifungal agents.
- Song, Ya-Li,Wu, Fan,Zhang, Chao-Chao,Liang, Guo-Chao,Zhou, Guan,Yu, Jiao-Jiao
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supporting information
p. 259 - 261
(2015/04/13)
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- Facile one-pot synthesis of some novel thiazolylpyrazole derivatives with antifungal activity
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A series of novel 1-(4-phenylthiazol-2-yl)-1,4-dihydrothiochroman[ 4,3-c]pyrazole have been prepared by a three-component reaction of thiochromanone-3-carbaldehyde, phenacyl bromide, and thiosemicarbazide. The reaction was in one-pot and did not require any additional catalyst with moderate yields. This method provided several advantages such as environment friendliness and simple work-up procedure. The compounds were assayed for antifungal activity and some of the new compounds can be further utilized as lead compounds.
- Song, Ya-Li,Yang, Tao,Dong, Yun-Fang,Wu, Fan,Yang, Geng-Liang
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supporting information
p. 134 - 136
(2014/01/23)
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- Copper-free asymmetric allylic alkylation of trisubstituted cyclic allyl bromides using grignard reagents
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AAA: The asymmetric allylic alkylation (AAA) of trisubstituted cyclic allyl bromides with Grignard reagents is catalytic (2 mol % of ligand) and regioselective (SN2'/SN2=91:9→100:0). The quaternary carbon centers are formed with good to high enantioselectivity (e.r.=81.5:19.5→96:4). Copyright
- Grassi, David,Alexakis, Alexandre
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supporting information
p. 13642 - 13646
(2014/01/06)
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- Synthesis and antifungal activity of some thiazole derivatives
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A series of some thiazole derivatives were designed and synthesized. The structure of newly synthesized compounds was characterized by HRMS, 1H NMR and 13C NMR. The synthesized compounds were evaluated against ten species of fungi in vitro by agar cup plate and micro-titration methods, respectively. The results of antifungal screening reveal that among all the compounds screened three compounds showed moderate antifungal activity. The MIC value of 3 h against two fungal strains C. neoformans and C. albicas is 8 μg mL-1 respectively. The MIC value of 3i against two fungal strains C. neoformans and T. mentagrophytes is 8 μg mL-1 and 16 μg mL-1, respectively and 3a against T. mentagrophytes is 16 μg mL-1, the MIC of others are all beyond 32 μg mL-1.
- Yang, Geng-Liang,Song, Ya-Li,Liu, Xiao-Ming,Yang, Ning
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p. 1849 - 1852
(2013/05/08)
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- Synthesis and antifungal activity of some novel (E)-2, 3-dihydro-3- [(phenylamino) methylene]-4H-1-benzothiopyran-4-ones
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A series of novel (E)-2,3-dihydro-3-[(phenylamino)methylene]-4H-1- benzothiopyran-4-ones has been synthesized by using 2,3-dihydro-4H-1- benzothiopyran-4-ones as the starting material. The structures of the new compounds are characterized by UV-vis, IR, HRMS, 1H NMR, and 13C NMR. 2D NMR spectroscopic studies revealed that at room temperature, these compounds rather exist in the keto-enamine than in the Schiff base form. The synthesized compounds were evaluated against two species of fungi in vitro by agar double dilution method. The results of antifungal screening revealed that the MIC value of (E)-8-chloro-2,3-dihydro-3-[(4- nitrophenylamino)methylene]-4H-1-benzothiopyran-4-one (4j) against Candida albicans is 32 μg·ml-1 while the control Fluconazole is 64 μg?ml-1.
- Liu, Xiao-Ming,Yang, Geng-Liang,Song, Ya-Li,Liu, Jie-Jie,Yang, Wang,Zhang, Dong-Nuan
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p. 228 - 234
(2013/07/26)
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- Synthesis and pharmacological evaluation of novel bisindolylalkanes analogues
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In an effort to develop potent anti-cancer chemopreventive agents that act on topoisomerase II, a novel series of bisindolylalkanes analogues such as 3,3′-(thiochroman-4,4-diyl)bis(1H-indole) are synthesized. Structures of all compounds are elucidated by 1H NMR, 13C NMR and HRMS. Anti-proliferative activities for all of these compounds are investigated by the method of MTT assay on 7 human cancer lines. Most of them showed antitumor activities in vitro, the half maximal inhibitory concentration (IC50) value is 7.798 μg/mL of 3a against MCF7. Compound 3a showed comparable topoisomerase II inhibitory activity to etoposide (VP-16) at 100 μM concentration. The rest of the compounds also showed varying degree topoisomerase II inhibitory activity.
- Song, Ya-Li,Dong, Yun-Fang,Yang, Tao,Zhang, Chao-Chao,Su, Li-Min,Huang, Xin,Zhang, Dong-Nuan,Yang, Geng-Liang,Liu, Yu-Xin
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p. 7624 - 7627
(2014/01/06)
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- Design and synthesis of α,β-epoxyketones as new anticancer agents
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As epoxy functional group has high anticancer activity, α,β-epoxyketones were designed and synthesized as new anticancer agents, and their structures were confirmed by UV, 1H NMR, IR, MS technigeces and elemental analysis. Their in vitro anticancer activities were evaluated by MTT method and the results showed that the compound 4c exhibited good activity with IC50 of 17.8, 22.0 and 24.1 μg/mL against A-549, Hela and HepG2 cells, respectively. The dose of LD50 of the mice by intragastric administration was 1864.4 mg/kg. Therefore, the α,β-epoxyketones could potentially provide as new anticancer agents. A series of α,β-epoxyketones were synthesized in a four steps reaction and tested for their anticancer activities.
- Ma, Zhengyue,Zhang, Xinghua,Wang, Shikui,He, Yang,Yang, Gengliang,Li, Beilei,Yang, Junjie,Lu, Yuejuan,Sun, Jiewei
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scheme or table
p. 757 - 764
(2011/11/12)
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- TRICYCLIC PYRAZOL AMINE DERIVATIVES
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This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.
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Page/Page column 124-125
(2011/06/16)
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- Nickel chloride hexahydrate: A novel reagent for Michael addition on α,β-unsaturated acids - A facile one-step route to 3-arylmercaptopropionic acids from thiophenols and α,β-unsaturated acids
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Michael additions have been successfully carried out in presence of a base, but when an α,β00-unsaturated acid is a substrate, it would be most unlikely for a carboxylate ion bearing α,β-unsaturated site to undergo a Michael addition. This problem has been circumvented in the present paper by carrying out a nickel chloride hexahydrate mediated Michael addition of thiophenols 1a-k on acrylic acid and on cinnamic acid to give 3-aryl mercaptopropionic acids 3a-k in excellent yield.
- Gogia, Santosh,Sirohi, Reenu,Gupta, Suman,Kishore,Joshi
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p. 1008 - 1011
(2007/10/03)
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