Synthesis and structure-activity relationships study of novel anti-tumor carbamate anhydrovinblastine analogues
Shao, Yong; Ding, Hong; Tang, Weidong; Lou, Liguang; Hu, Lihong
刊名BIOORGANIC & MEDICINAL CHEMISTRY
2007-08-01
卷号15期号:15页码:5061-5075
关键词antitumor anhydrovinblastine derivatives carbamate cytotoxicity
ISSN号0968-0896
DOI10.1016/j.bmc.2007.05.045
文献子类Article
英文摘要A series of 3-demethoxycarbonyl-3-carbamate methyl anhydrovinblastine derivatives (compounds 8b-32b) were designed, synthesized, and evaluated for their inhibition activities against human non-small cell lung cancer cell line (A549) and a human cervix epithelial adenocarcinoma cell line (HeLa). The structure-activity relationships of this new series are described in this paper. Cytotoxicity data revealed that the size of substituents and substitution position had important influence on cytotoxic activity. On two cell lines, compounds (8b and 30b) had more potent cytotoxic activity than the lead compound (le, AVLB). The preliminary antitumor studies of 8b in vivo showed that it might be promising for the development of new antitumor agents. (c) 2007 Elsevier Ltd. All rights reserved.
WOS关键词VINCA ALKALOIDS ; CLINICAL DEVELOPMENT ; CATHARANTHUS-ROSEUS ; DERIVATIVES ; VINDOLINE ; VINFLUNINE
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种英语
出版者PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号WOS:000247714900002
内容类型期刊论文
源URL[http://119.78.100.183/handle/2S10ELR8/273183]  
专题药理学第一研究室
上海中药现代化研究中心
通讯作者Lou, Liguang
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Pharmacol, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai 201203, Peoples R China
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Shao, Yong,Ding, Hong,Tang, Weidong,et al. Synthesis and structure-activity relationships study of novel anti-tumor carbamate anhydrovinblastine analogues[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2007,15(15):5061-5075.
APA Shao, Yong,Ding, Hong,Tang, Weidong,Lou, Liguang,&Hu, Lihong.(2007).Synthesis and structure-activity relationships study of novel anti-tumor carbamate anhydrovinblastine analogues.BIOORGANIC & MEDICINAL CHEMISTRY,15(15),5061-5075.
MLA Shao, Yong,et al."Synthesis and structure-activity relationships study of novel anti-tumor carbamate anhydrovinblastine analogues".BIOORGANIC & MEDICINAL CHEMISTRY 15.15(2007):5061-5075.
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