Bakuchiol derivatives as novel and potent cytotoxic agents: a report

Eur J Med Chem. 2012 Mar:49:55-67. doi: 10.1016/j.ejmech.2011.12.018.

Rabiya Majeed ¹, Mallepally V Reddy, Praveen K Chinthakindi, Payare L Sangwan, Abid Hamid, Gousia Chashoo, Ajit K Saxena, Surrinder Koul

Affiliations

Affiliation

1 Bioorganic Chemistry Section, CSIR-Indian Institute of Integrative Medicine, Jammu, India.

PMID: 22245048 DOI: 10.1016/j.ejmech.2011.12.018

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.

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