DERIVATIVES OF A NOVEL CYCLOPEPTOLIDE .2. SYNTHESIS, ACTIVITY AGAINST MULTIDRUG-RESISTANCE IN CHO AND KB CELLS IN-VITRO, AND STRUCTURE-ACTIVITY-RELATIONSHIPS

被引：15
|
作者：
EMMER, G
GRASSBERGER, MA
SCHULZ, G
BOESCH, D
GAVERIAUX, C
LOOR, F
机构：
[1] SANDOZ PHARMA AG, PRECLIN RES, DEPT BIOTECHNOL, CH-4002 BASEL, SWITZERLAND
[2] UNIV LOUIS PASTEUR STRASBOURG 1, FAC PHARM, IMMUNOL LAB, F-67401 ILLKIRCH GRAFFENSTADEN, FRANCE
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 1994年 / 37卷 / 13期
关键词：
D O I：
10.1021/jm00039a003
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of derivatives of the novel cyclopeptolide 1 was prepared, and their ability to chemosensitize multi drug resistant CHO and KB cells in vitro was evaluated. In contrast to the parent compound, several of the derivatives were found to be highly active. In particular, conversion of the R-lactic acid residue of 1 into its S-isomer via lactone ring cleavage and recyclization with inversion resulted in a marked enhancement of activity. Some of these derivatives (e.g., 15a, SDZ 280.446) belong to the most potent resistance modulating compounds known so far.
引用
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页码：1918 / 1928
页数：11
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