European Journal of Medicinal Chemistry 2012-03-01

Bakuchiol derivatives as novel and potent cytotoxic agents: a report.

Rabiya Majeed, Mallepally V Reddy, Praveen K Chinthakindi, Payare L Sangwan, Abid Hamid, Gousia Chashoo, Ajit K Saxena, Surrinder Koul

Index: Eur. J. Med. Chem. 49C , 55-67, (2012)

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Abstract

A library of 28 compounds comprising of acyl, amino, halo, nitro, styryl and cyclized derivatives of bakuchiol have been evaluated against a panel of eight human cancer cell lines. Bioevaluation studies have resulted in the identification of potent cytotoxic molecules exhibiting concentration dependent growth inhibition against leukemia cancer cells with best results observed for compounds 17 and 22 exhibiting IC(50) 1.8 and 2.0 μM respectively. As evident from various biological end-points, inhibition of cell proliferation by inducing G2/M cell cycle arrest, mitochondrial membrane disruption followed by DNA fragmentation and apoptosis is demonstrated.Copyright © 2011 Elsevier Masson SAS. All rights reserved.