Synthesis, DNA-binding ability and evaluation of antitumour activity of triazolo[1,2,4] benzothiadiazine linked pyrrolo[2,1-c] [1,4] benzodiazepine conjugates

被引：42

作者：

Kamal, Ahmed ^{[1
]}

Khan, M. Naseer A. ^{[1
]}

Srikanth, Y. V. V. ^{[1
]}

Reddy, K. Srinivasa ^{[1
]}

Juvekar, Aarti ^{[2
]}

Sen, Subrata ^{[2
]}

Kurian, Nisha ^{[2
]}

Zingde, Surekha ^{[2
]}

机构：

[1] Indian Inst Chem Technol, Div Organ Chem, Biol Chem Lab, Hyderabad 500007, Andhra Pradesh, India

[2] Adv Ctr Treatment Res & Educ Canc, Navi Mumbai 410210, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 16期

关键词：

triazolobenzothiadiazines; pyrrolobenzodiazepine; antitumour activity; DNA-binding ability;

D O I：

10.1016/j.bmc.2008.06.056

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 triazolobenzothiadiazine-pyrrolobenzodiazepine conjugates linked through different alkane spacers have been prepared. These compounds have exhibited significant cytotoxicity against most of the cell lines examined. Compound 5a displays GI(50) values from 1.83 to 2.38 mu M against seven human tumour cell lines, and is identified as a promising lead compound from this series. Their DNA thermal denaturation studies have also been carried out, and one of the compounds 5c elevates the DNA helix melting temperature of the CT-DNA by 2.6 degrees C after incubation for 36 h. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：7804 / 7810

页数：7

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