Synthesis of 1,2,3-triazole-linked pyrrolobenzodiazepine conjugates employing 'click' chemistry: DNA-binding affinity and anticancer activity

  • Bioorg Med Chem Lett. 2008 Feb 15;18(4):1468-73. doi: 10.1016/j.bmcl.2007.12.063.
Ahmed Kamal  1 ,  N Shankaraiah ,  V Devaiah ,  K Laxma Reddy ,  Aarti Juvekar ,  Subrata Sen ,  Nisha Kurian ,  Surekha Zingde
Affiliations
  • 1. Biotransformation Laboratory, Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 007, India.
PMID: 18207392 DOI: 10.1016/j.bmcl.2007.12.063
Abstract

1,2,3-Triazole based molecules are useful pharmacophores for several DNA-alkylating and cross-linking agents. A series of A/C8, C/C2 and A/C8-C/C2-linked 1,2,3-triazole-PBD conjugates have been synthesized by employing 'click' chemistry. These molecules have exhibited promising DNA-binding affinity and Anticancer activity in selected human Cancer cell lines.