Remarkable DNA binding affinity and potential anticancer activity of pyrrolo[2,1-c][1,4]benzodiazepine-naphthalimide conjugates linked through piperazine side-armed alkane spacers

被引:49
作者
Kamal, Ahmed [1 ]
Ramu, R. [1 ]
Tekumalla, Venkatesh [1 ]
Khanna, G. B. Ramesh [1 ]
Barkume, Madan S. [2 ]
Juvekar, Aarti S. [2 ]
Zingde, Surekha M. [2 ]
机构
[1] Indian Inst Chem Technol, Div Organ Chem, Hyderabad 500607, Andhra Pradesh, India
[2] Tata Mem Ctr Khargar, Adv Ctr Treatment Res & Educ Canc, Navi Mumbai 410210, India
关键词
pyrrolobenzodiazepines; naphthalimides; piperazine ring; DNA binding affinity; anticancer activity;
D O I
10.1016/j.bmc.2008.06.034
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
A series of pyrrolobenzodiazepine-naphthalimide conjugates tethered through a piperazine ring system have been designed, synthesized, and evaluated for their anticancer activity. These new conjugates exhibit very high DNA binding affinity and cytotoxic activity against a number of cell lines. (C) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码:7218 / 7224
页数:7
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