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

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

  • Bioorg Med Chem. 2008 Aug 15;16(16):7804-10. doi: 10.1016/j.bmc.2008.06.056.
Ahmed Kamal 1,  M Naseer A Khan,  Y V V Srikanth,  K Srinivasa Reddy,  Aarti Juvekar,  Subrata Sen,  Nisha Kurian,  Surekha Zingde
Affiliations

Affiliation

  • 1 Chemical Biology Laboratory, Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 007, India. ahmedkamal@iict.res.in
PMID: 18657979 DOI: 10.1016/j.bmc.2008.06.056
Abstract

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.

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