title: 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.affiliation: Bioorganic Chemistry Section, CSIR-Indian Institute of Integrative Medicine, Jammu, India.
authors.forename: Rabiya
authors.initials: R
authors.lastname: Majeed
authors.forename: Mallepally V
authors.initials: MV
authors.lastname: Reddy
authors.forename: Praveen K
authors.initials: PK
authors.lastname: Chinthakindi
authors.forename: Payare L
authors.initials: PL
authors.lastname: Sangwan
authors.forename: Abid
authors.initials: A
authors.lastname: Hamid
authors.forename: Gousia
authors.initials: G
authors.lastname: Chashoo
authors.forename: Ajit K
authors.initials: AK
authors.lastname: Saxena
authors.forename: Surrinder
authors.initials: S
authors.lastname: Koul
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000494:pharmacology*; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D053938:DNA Fragmentation / Q000187:drug effects; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000235:genetics / Q000378:metabolism; D010636:Phenols / Q000737:chemistry* / Q000494:pharmacology*; D029907:Psoralea / Q000737:chemistry*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D010636:Phenols; C012765:bakuchiol