中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
首页 机构 成果 学者
  
  1. CAS IR Grid
  2. 上海药物研究所
  3. 中国科学院上海药物研究所
  4. 药物化学研究室
Synthesis and Anticancer Activity of 7,8-dihydroxy-4-arylcoumarins

文献类型：期刊论文

作者Wu, Jianrui1; Peng, Ting2; Chen, Fang1; Leng, Yixin1; Tong, Linjiang2; Li, Mengyuan2; Qu, Rong2; Xie, Hua2; Ding, Jian2; Duan, Wenhu1
刊名LETTERS IN DRUG DESIGN & DISCOVERY
出版日期2015
卷号12期号:5页码:366-373
关键词Anticancer 4-Arylcoumarin Cytotoxicity Structure-activity relationship Tubulin Tyrosine kinase inhibition
ISSN号1570-1808
DOI10.2174/1570180812666141111235026
文献子类Article
英文摘要A series of 7,8-dihydroxy-4-arylcoumarins, the derivatives related to DW532 that was an anti-tumor agent targeting both kinase and tubulin, was prepared by Suzuki coupling reaction. Among them, compounds 6a, 6b, and 6c were found to exhibit anti-proliferation activities against human breast carcinoma MDA-MB-468 cells with IC50 values of 0.64, 0.69, and 1.33 mu M, respectively and human epidermoid carcinoma A431 cells with IC50 values of 2.56, 1.78, and 2.29 mu M, respectively. Further evaluation of the selected molecules revealed that they displayed broad-spectrum inhibitory activities against a panel of kinases including Flt-1, VEGFR2, RET, EGFR, etc. In vitro tubulin polymerization assay and molecular docking indicated that the substitution of 3'-OH and 4'-OCH3 on the 4-phenyl ring was essential to achieve potent tubulin inhibition.
WOS关键词BIOLOGICAL EVALUATION ; 4-SUBSTITUTED COUMARINS ; 4-ARYLCOUMARIN ANALOGS ; DERIVATIVES ; INHIBITORS ; 4-PHENYLCOUMARINS ; CONSTITUENTS
资助项目Chinese National Natural Science Foundation[81273365] ; Chinese National Natural Science Foundation[81173080] ; Chinese National Natural Science Foundation[81321092] ; Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program''[2012ZX09103101-024] ; Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program''[2014ZX09304002] ; Chinese National Programs for High Technology Research and Development[2012AA020302] ; Shanghai Science and Technology Commission[12DZ1930802]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000351780700004
出版者BENTHAM SCIENCE PUBL LTD
源URL[http://119.78.100.183/handle/2S10ELR8/276742]  
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Xie, Hua
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, Shanghai 201203, Peoples R China;
2.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Wu, Jianrui,Peng, Ting,Chen, Fang,et al. Synthesis and Anticancer Activity of 7,8-dihydroxy-4-arylcoumarins[J]. LETTERS IN DRUG DESIGN & DISCOVERY,2015,12(5):366-373.
APA Wu, Jianrui.,Peng, Ting.,Chen, Fang.,Leng, Yixin.,Tong, Linjiang.,...&Duan, Wenhu.(2015).Synthesis and Anticancer Activity of 7,8-dihydroxy-4-arylcoumarins.LETTERS IN DRUG DESIGN & DISCOVERY,12(5),366-373.
MLA Wu, Jianrui,et al."Synthesis and Anticancer Activity of 7,8-dihydroxy-4-arylcoumarins".LETTERS IN DRUG DESIGN & DISCOVERY 12.5(2015):366-373.

入库方式： OAI收割

来源：上海药物研究所

浏览0
下载0
收藏0
其他版本

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。