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Synthesis and biological evaluation of anilino substituted pyrimidine linked pyrrolobenzodiazepines as potential anticancer agents.

Bioorganic & medicinal chemistry letters 2010 Jul 27; In press

Link to PubMed abstract

Kamal A, Reddy J JS, Ramaiah M MJ, Bharathi E EV, Dastagiri D, Reddy M MK, Pushpavalli S SN, Pal-Bhadra M

Division of Organic Chemistry, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 607, India.

A series of new anilino substituted pyrimidine linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates were prepared and evaluated for their anticancer activity. The effects of four promising PBD conjugates on cell cycle of cancerous cell line A375 were investigated. These compounds showed the characteristic features of apoptosis like enhancement in the levels of p53, release of cytochrome c, and cleavage of PARP.