2. Academic Validation
  3. Synthesis and biological evaluation of estradiol linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates as potential anticancer agents

Synthesis and biological evaluation of estradiol linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates as potential anticancer agents

  • Bioorg Med Chem. 2011 Apr 15;19(8):2565-81. doi: 10.1016/j.bmc.2011.03.015.
Ahmed Kamal 1,  M Kashi Reddy,  M Janaki Ramaiah,  Rajender,  J Surendranadha Reddy,  Y V V Srikanth,  D Dastagiri,  E Vijaya Bharathi,  S N C V L Pushpavalli,  Pranjal Sarma,  Manika Pal-Bhadra
Affiliations

Affiliation

  • 1 Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad, India. ahmedkamal@iict.res.in
PMID: 21459581 DOI: 10.1016/j.bmc.2011.03.015
Abstract

A series of new estradiol linked pyrrolo[2,1-c][1,4]benzodiazepine (E(2)-PBD) conjugates (3a-f, 4a-f and 5a-f) with different linker architectures including a triazole moiety have been designed and synthesized. All the 18 compounds have been evaluated for their Anticancer activity and it is observed that some of the compounds particularly 4c-e and 5c,d exhibited significant Anticancer activity. The detailed biological aspects relating to the cell cycle effects and tubulin depolymerization activity have been examined with a view to understand the mechanism of action of these conjugates. Among all these conjugates, one of the compound 5c could be considered as the most effective compound particularly against MCF-7 breast Cancer cell line.

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