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

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.

• Authors: Rabiya Majeed, Mallepally V Reddy, Praveen K Chinthakindi, Payare L Sangwan, Abid Hamid, Gousia Chashoo, Ajit K Saxena, Surrinder Koul
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 49 Pg. 55-67 (Mar 2012) ISSN: 1768-3254 [Electronic] France
• PMID: 22245048 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2011 Elsevier Masson SAS. All rights reserved.

Chemical References

• Antineoplastic Agents, Phytogenic
• Phenols
• bakuchiol

Topics

• Antineoplastic Agents, Phytogenic (chemistry, pharmacology)
• Cell Cycle Checkpoints (drug effects)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• DNA Fragmentation (drug effects)
• Humans
• Neoplasms (drug therapy, genetics, metabolism)
• Phenols (chemistry, pharmacology)
• Psoralea (chemistry)