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

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• 作者：Ahmed Kamal ; M. Naseer A. Khan ; Y.V.V. Srikanth ; K. Srinivasa Reddy ; Aarti Juvekar ; Subrata Sen ; Nisha Kurian ; Surekha Zingde
• 关键词：Triazolobenzothiadiazines ; Pyrrolobenzodiazepine ; Antitumour activity ; DNA-binding ability
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2008
• 出版时间：15 August 2008
• 年：2008
• 卷：16
• 期：16
• 页码：7804-7810
• 全文大小：212 K

文摘

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 GI₅₀ values from 1.83 to 2.38 μM 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 °C after incubation for 36 h.