Semi-synthesis and biological activity of γ-lactones analogs of camptothecin

被引：14

作者：

Li, Mingzong ^{[2
]}

Tang, Weidong ^{[1
]}

Zeng, Fuxing ^{[2
]}

Lou, Liguang ^{[1
]}

You, Tianpa ^{[2
]}

机构：

[1] Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China

[2] Univ Sci & Technol China, Dept Chem, Hefei 230026, Anhui, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 24期

关键词：

Camptothecin; Camptothecin derivatives; Semi-synthesis; Antitumor activity; Topoisomerase I;

D O I：

10.1016/j.bmcl.2008.10.074

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of E-ring gamma-lactone camptothecin derivatives were synthesized by semi-synthesis via a three-step domino reaction. Their biological activity was evaluated on two types of human tumor cell lines A549 and HT-29 with sulforhodamine-B (SRB) method. The antitumor activity of these compounds was lower than SN-38, only compound 12c was found to be close to the activity of Topotecan. The structure-activity relationship (SAR) of these analogs was studied and discussed. Crown Copyright (C) 2008 Published by Elsevier Ltd. All rights reserved.

引用

页码：6441 / 6443

页数：3

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