Article ID Journal Published Year Pages File Type
1392977 European Journal of Medicinal Chemistry 2012 13 Pages PDF
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 IC50 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.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Synthesis of 28 bakuchiol derivatives. ► Several derivatives were active against various human cancer cell lines. ► The molecules work as inducers of apoptosis.

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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