Kamal Ahmed, Khan M Naseer A, Srikanth Y V V, Reddy K Srinivasa, Juvekar Aarti, Sen Subrata, Kurian Nisha, Zingde Surekha
Chemical Biology Laboratory, Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 007, India.
Bioorg Med Chem. 2008 Aug 15;16(16):7804-10. doi: 10.1016/j.bmc.2008.06.056. Epub 2008 Jul 3.
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 microM 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.
已经制备了一系列通过不同烷烃间隔基连接的三唑并苯并噻二嗪-吡咯并苯并二氮杂䓬共轭物。这些化合物对大多数所检测的细胞系都表现出显著的细胞毒性。化合物5a对七种人类肿瘤细胞系的GI(50)值在1.83至2.38微摩尔之间，并且被确定为该系列中有前景的先导化合物。还对它们进行了DNA热变性研究，其中一种化合物5c在孵育36小时后使CT-DNA的DNA螺旋解链温度升高了2.6摄氏度。
