title: Synthesis and biological evaluation of novel 1,6-diaryl pyridin-2(1H)-one analogs.
abstract: A series of 1,6-diaryl pyridin-2(1H)-one analogs were designed and synthesized via consecutive Chan-Lam coupling and Suzuki coupling. These novel compounds were evaluated for their antiproliferative activity against two tumor cell lines (SKOV-3 and HepG2). Compounds 1b, 1c, 1e and 1f displayed comparable in vitro cytotoxicity with taxol, while their in vivo antitumor activity was less effective than taxol. In addition, cell cycle assay indicated that these 1,6-diaryl pyridin-2(1H)-one compounds induced cell cycle arrest in the G1/M phase in the HepG2 cell line.
authors.affiliation: Department of Chemistry, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, China.
authors.forename: Taijie
authors.initials: T
authors.lastname: Chen
authors.forename: Yu
authors.initials: Y
authors.lastname: Luo
authors.forename: Youhong
authors.initials: Y
authors.lastname: Hu
authors.forename: Bo
authors.initials: B
authors.lastname: Yang
authors.forename: Wei
authors.initials: W
authors.lastname: Lu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D056945:Hep G2 Cells; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology; D011728:Pyridones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D011728:Pyridones