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
收藏
页码：2595 / 2599
页数：5
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