Synthesis and biological evaluation of estradiol linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates as potential anticancer agents |
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Authors: | Kamal Ahmed Reddy M Kashi Ramaiah M Janaki Rajender Reddy J Surendranadha Srikanth Y V V Dastagiri D Bharathi E Vijaya Pushpavalli S N C V L Sarma Pranjal Pal-Bhadra Manika |
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Affiliation: | Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad, India. ahmedkamal@iict.res.in |
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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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