1,2,4-benzothiadiazine linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates: synthesis, DNA-binding affinity and cytotoxicity

  • Bioorg Med Chem Lett. 2007 Oct 1;17(19):5345-8. doi: 10.1016/j.bmcl.2007.08.018.
Ahmed Kamal  1 ,  M Naseer A Khan ,  K Srinivasa Reddy ,  S Kaleem Ahmed ,  M Shiva Kumar ,  Aarti Juvekar ,  Subrata Sen ,  Surekha Zingde
Affiliations
  • 1. Biotransformation Laboratory, Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 007, India. [email protected]
PMID: 17723301 DOI: 10.1016/j.bmcl.2007.08.018
Abstract

Benzothiadiazine-pyrrolobenzodiazepine conjugates linked through different alkane spacers have been prepared. These new classes of hybrid molecules exhibit cytotoxicity against many Cancer cell lines. Their DNA thermal denaturation studies have been carried out and one of the compounds (4b) elevates the DNA helix melting temperature of the CT-DNA by 6.7 degrees C after incubation for 36 h.