SYNTHESIS AND IN-VITRO CYTOTOXICITY OF DIASTEREOISOMERICALLY MODIFIED DOLASTATIN-15 ANALOGS

被引:8
作者
ROUX, F
GALEOTTI, N
PONCET, J
JOUIN, P
CROS, S
ZENKE, G
机构
[1] LAB MECANISMES MOLEC COMMUN CELLULAIRES,F-34094 MONTPELLIER 5,FRANCE
[2] CNRS,PHARMACOL & TOXICOL FONDAMENTALES LAB,F-31077 TOULOUSE,FRANCE
[3] SANDOZ PHARMA LTD,CH-4002 BASEL,SWITZERLAND
关键词
DOLASTATIN; DEPSIPEPTIDE; CYTOSTATIC ACTIVITY; ANTIPROLIFERATIVE EFFECT;
D O I
10.1016/S0960-894X(01)80540-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Dolastatin 15 1(4S,7S) is a potent cytostatic depsipeptide of marine origin. Analysis of the effects of the stereochemistry in the non-peptide moiety on activity revealed that chirality inversion in the aromatic terminal region preserves the antiproliferative activity.
引用
收藏
页码:1947 / 1950
页数:4
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