Synthesis, biological evaluation and DNA binding properties of novel bleomycin analogues

被引：14

作者：

Xu, ZD ^{[1
]}

Wang, M ^{[1
]}

Xiao, SL ^{[1
]}

Liu, CL ^{[1
]}

Yang, M ^{[1
]}

机构：

[1] Peking Univ, Natl Res Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(03)00435-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of bleomycin analogues was prepared with a facile synthetic method. All the compounds were shown to display significant antitumor activity against HeLa and BGC-823 cell lines in vitro. The binding properties with CT-DNA and cleavage efficiency to pBR322 DNA were investigated, the results indicate that there is a positive relationship between DNA cleavage efficiency and the binding affinity to DNA, and the antitumor activity of the bleomycin analogues is enhanced as the hydrophobicity of the C-terminus substituent side chain increased. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：2595 / 2599

页数：5

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