Synthesis and biological evaluation of 6H-pyrido[2 ',1 ':2,3] imidazo[4,5-c] isoquinolin-5(6H)-ones as antimitotic agents and inhibitors of tubulin polymerization
文献类型：期刊论文
| 作者 | Meng, Tao2 ; Wang, Wei1; Zhang, Zhixiang1; Ma, Lanping2; Zhang, Yongliang2; Miao, Zehong1; Shen, Jingkang2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2014-01-15 |
| 卷号 | 22期号:2页码:848-855 |
| 关键词 | 6H-Pyrido[2 ',1 ':2,3]imidazo[4,5-c] isoquinolin-5(6H)-ones Antitumor agents Inhibitors of tubulin polymerization Colchicine binding site |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2013.12.004 |
| 文献子类 | Article |
| 英文摘要 | A series of 6H-pyrido[20,10: 2,3] imidazo[4,5-c] isoquinolin-5(6H)-ones have been synthesized and evaluated for their antiproliferative activities. Among them, compounds 2j and 4d displayed potent cytotoxic activities in vitro against HeLa cell line with IC50 values of 0.07 and 0.06 mu M, respectively. In general, the antiproliferative activities are correlated with the inhibitory effect on tubulin polymerization and binding property of the colchicine binding site. In addition, flow cytometry and immunofluorescence analysis revealed selected compounds caused G2/M phase arrest of the cell cycle and disruption of the mitotic spindle assembly, which had correlation with proliferation inhibitory activity. (C) 2014 Published by Elsevier Ltd. |
| WOS关键词 | MICROTUBULE INHIBITORS ; MITOTIC SPINDLE ; BINDING ; COLCHICINE ; CELLS ; APOPTOSIS ; MITOSIS ; DRUGS ; SITE |
| 资助项目 | National Science & Technology Major Project 'Key New Drug Creation and Manufacturing Program', China[2012ZX09103-101-026] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000329576400019 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277228]  |
| 专题 | 药物化学研究室 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 |
| 通讯作者 | Ma, Lanping |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Div Med Chem, State Key Lab Drug Res, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Meng, Tao,Wang, Wei,Zhang, Zhixiang,et al. Synthesis and biological evaluation of 6H-pyrido[2 ',1 ':2,3] imidazo[4,5-c] isoquinolin-5(6H)-ones as antimitotic agents and inhibitors of tubulin polymerization[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2014,22(2):848-855. |
| APA | Meng, Tao.,Wang, Wei.,Zhang, Zhixiang.,Ma, Lanping.,Zhang, Yongliang.,...&Shen, Jingkang.(2014).Synthesis and biological evaluation of 6H-pyrido[2 ',1 ':2,3] imidazo[4,5-c] isoquinolin-5(6H)-ones as antimitotic agents and inhibitors of tubulin polymerization.BIOORGANIC & MEDICINAL CHEMISTRY,22(2),848-855. |
| MLA | Meng, Tao,et al."Synthesis and biological evaluation of 6H-pyrido[2 ',1 ':2,3] imidazo[4,5-c] isoquinolin-5(6H)-ones as antimitotic agents and inhibitors of tubulin polymerization".BIOORGANIC & MEDICINAL CHEMISTRY 22.2(2014):848-855. |
入库方式： OAI收割
来源：上海药物研究所
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