Potent Antitumor Activities and Structure Basis of the Chiral beta-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin
文献类型：期刊论文
| 作者 | Zhou, Pengfei1; Liu, Yan2; Zhou, Lu1; Zhu, Kongkai2; Feng, Kechang1; Zhang, Hao2; Liang, Yuru1; Jiang, Hualiang2 ; Luo, Cheng2; Liu, Mingming1
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| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2016-11-24 |
| 卷号 | 59期号:22页码:10329-10334 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/acs.jmedchem.6b01268 |
| 文献子类 | Article |
| 英文摘要 | A series of chiral,beta-lactam bridged analogues (3-substituted 1,4-diaryl-2-azetidinones) of combretastatin A-4 (CA-4) were synthesized asymmetrically, and their antitumor activities were evaluated in vitro and in vivo. The cocrystal structure of tubulin in complex with compound 9 was determined by X-ray crystallography, which showed that 9 binds to the same site as colchicine with similar binding mode, and the absolute configuration of its C-4 was first identified and demonstrated to be critically important for their antiproliferative activities. |
| WOS关键词 | ASYMMETRIC ALLYLIC AMINATION ; BAYLIS-HILLMAN ADDUCTS ; ANTICANCER AGENTS ; BIOLOGICAL EVALUATION ; INHIBITORS ; MECHANISM ; INTERACT ; LIGANDS ; SITE |
| 资助项目 | National Natural Science Foundation of China[21472025] ; National Natural Science Foundation of China[81302257] ; National Natural Science Foundation of China[21472208] ; National Natural Science Foundation of China[81625022] ; National Natural Science Foundation of China[81430084] ; National Natural Science Foundation of China[21210003] ; National Basic Research Program[2015CB910304] ; Fund of State Key Laboratory of Toxicology and Medical Countermeasures, Academy of Military Medical Science[TMC201505] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000388913200024 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275799]  |
| 专题 | 药物发现与设计中心 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 |
| 通讯作者 | Luo, Cheng; Liu, Mingming; Wang, Yang |
| 作者单位 | 1.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhou, Pengfei,Liu, Yan,Zhou, Lu,et al. Potent Antitumor Activities and Structure Basis of the Chiral beta-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin[J]. JOURNAL OF MEDICINAL CHEMISTRY,2016,59(22):10329-10334. |
| APA | Zhou, Pengfei.,Liu, Yan.,Zhou, Lu.,Zhu, Kongkai.,Feng, Kechang.,...&Wang, Yang.(2016).Potent Antitumor Activities and Structure Basis of the Chiral beta-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin.JOURNAL OF MEDICINAL CHEMISTRY,59(22),10329-10334. |
| MLA | Zhou, Pengfei,et al."Potent Antitumor Activities and Structure Basis of the Chiral beta-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin".JOURNAL OF MEDICINAL CHEMISTRY 59.22(2016):10329-10334. |
入库方式： OAI收割
来源：上海药物研究所
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