Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors
文献类型：期刊论文
| 作者 | Zhang, Xuan2 ; Kong, Yannan3; Zhang, Jie1; Su, Mingbo4; Zhou, Yubo4; Zang, Yi4; Li, Jia4; Chen, Yi1; Fang, Yanfen3; Zhang, Xiongwen3
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2015-05-05 |
| 卷号 | 95页码:127-135 |
| 关键词 | Colchicine Dual inhibitor HDAC Tubulin Hybrid |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2015.03.035 |
| 文献子类 | Article |
| 英文摘要 | A new class of colchicine derivatives were designed and synthesized as tubulin-HDAC dual inhibitors. Biological evaluations of these hybrids included the inhibitory activity of HDAC, tubulin polymerization analysis, in vitro cell cycle analysis in HCT-116 cells and cytotoxicity against different cancer cell lines. Hybrid 6d behaved as potent HDAC-tubulin dual inhibitor and showed comparable cytotoxicity with colchicine. Compound ha exhibited powerful tubulin inhibitory activity, moderate anti-HDAC activity and the most potent cytotoxicity (IC50 = 2-105 nM). (C) 2015 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | GROWTH-FACTOR RECEPTOR ; T-CELL LYMPHOMA ; CANCER-CELLS ; POTENT INHIBITORS ; INDUCED APOPTOSIS ; ANTICANCER DRUGS ; IN-VIVO ; DISCOVERY ; THERAPY ; VORINOSTAT |
| 资助项目 | National Natural Science Foundation of China[81172936] ; National Natural Science Foundation of China[81173033] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000354139900012 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276536]  |
| 专题 | 国家新药筛选中心 中国科学院上海药物研究所 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药理学第一研究室 药物安全性评价中心 |
| 通讯作者 | Fang, Yanfen |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.E China Normal Univ, Inst Drug Discovery & Dev, Shanghai 200062, Peoples R China; 3.E China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai 200062, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Xuan,Kong, Yannan,Zhang, Jie,et al. Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2015,95:127-135. |
| APA | Zhang, Xuan.,Kong, Yannan.,Zhang, Jie.,Su, Mingbo.,Zhou, Yubo.,...&Lu, Wei.(2015).Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,95,127-135. |
| MLA | Zhang, Xuan,et al."Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 95(2015):127-135. |
入库方式： OAI收割
来源：上海药物研究所
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