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通过哌嗪侧链烷烃间隔基连接的吡咯并[2,1-c][1,4]苯并二氮杂卓-萘二甲酰亚胺共轭物具有显著的DNA结合亲和力和潜在的抗癌活性。

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.

作者信息

Kamal Ahmed, Ramu R, Tekumalla Venkatesh, Khanna G B Ramesh, Barkume Madan S, Juvekar Aarti S, Zingde Surekha M

机构信息

Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 607, India.

出版信息

Bioorg Med Chem. 2008 Aug 1;16(15):7218-24. doi: 10.1016/j.bmc.2008.06.034. Epub 2008 Jun 25.

Abstract

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.

摘要

设计、合成了一系列通过哌嗪环系统连接的吡咯并苯并二氮杂卓-萘二甲酰亚胺缀合物,并对其抗癌活性进行了评估。这些新的缀合物对多种细胞系表现出非常高的DNA结合亲和力和细胞毒性活性。

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