Synthesis and biological evaluation of estradiol linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates as potential anticancer agents
2011; Elsevier BV; Volume: 19; Issue: 8 Linguagem: Inglês
10.1016/j.bmc.2011.03.015
ISSN1464-3391
AutoresÄhmed Kamal, M. Kashi Reddy, M. Janaki Ramaiah, Rajender, Jhansi Reddy, Y. V. V. Srikanth, D. Dastagiri, E. Vijaya Bharathi, S. N. C. V. L. Pushpavalli, P.N. Sarma, Manika Pal‐Bhadra,
Tópico(s)Cancer Treatment and Pharmacology
ResumoA series of new estradiol linked pyrrolo[2,1-c][1,4]benzodiazepine (E2-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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