Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents

被引：29

作者：

O'Connell, CE ^{[1
]}

Salvato, KA ^{[1
]}

Meng, ZY ^{[1
]}

Littlefield, BA ^{[1
]}

Schwartz, CE ^{[1
]}

机构：

[1] Eisai Res Inst, Andover, MA 01810 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(99)00243-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The marine natural product hapalosin and 22 analogs, which incorporated systematic substituent deletions or variations, were prepared. These compounds were evaluated in a cell-based assay for both MDR-reversing activity and general cytotoxicity. Some substituent modifications resulted in lower cytotoxicities, but most structural changes were either detrimental to or did not seriously alter the MDR-reversing activity. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：1541 / 1546

页数：6

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