Synthesis of C8-linked pyrrolo[2,1-c][1,4]benzodiazepine-benzimidazole conjugates with remarkable DNA-binding affinity

被引:33
作者
Kamal, A [1 ]
Ramulu, P [1 ]
Srinivas, O [1 ]
Ramesh, G [1 ]
Kumar, PP [1 ]
机构
[1] Indian Inst Chem Technol, Div Organ Chem, Hyderabad 500007, Andhra Pradesh, India
关键词
pyrrolobenzodiazepine; benzimidazoles; hoechst-33258; DNA-binding ability; cytotoxicity;
D O I
10.1016/j.bmcl.2004.06.069
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Two types of benzimidazoles have been synthesized and linked to DC-81 at C8-position through different alkyl chain spacers. These PBD conjugates have exhibited remarkable DNA-binding affinity, and a representative compound shows promising in vitro anticancer activity. (C) 2004 Published by Elsevier Ltd.
引用
收藏
页码:4791 / 4794
页数:4
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