Synthesis and evaluation of a novel E-ring modified α-hydroxy keto ether analogue of camptothecin

被引：27

作者：

Du, W

Curran, DP ^{[1
]}

Bevins, RL

Zimmer, SG

Zhang, JH

Burke, TG

机构：

[1] Univ Pittsburgh, Dept Chem, Pittsburgh, PA 15260 USA

[2] Univ Kentucky, Coll Pharm, Lexington, KY 40506 USA

[3] Univ Kentucky, Coll Med, Lexington, KY 40506 USA

[4] Univ Kentucky, Lucille P Markey Canc Ctr, Expt Therapeut Program, Lexington, KY 40506 USA

[5] Tigen Pharmaceut Inc, Lexington, KY 40506 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2002年 / 10卷 / 01期

关键词：

D O I：

10.1016/S0968-0896(01)00252-8

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis of a novel E-ring modified keto ether analogue of camptothecin and homocamptothecin by the cascade radical annulation route is reported. The analogue, Du1441, is an isomer of homocamptothecin, but includes the a-hydroxy carbonyl functionality that camptothecin possesses and homocamptothecin lacks. Despite these similarities, the new keto ether analogue is inactive in cell assays, and implications for the structure/activity relationship are discussed. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：103 / 110

页数：8

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