title: Synthesis and antiproliferative activity of novel diaryl ureas possessing a 4H-pyrido[1,2-a]pyrimidin-4-one group.
abstract: We herein disclose a series of novel diaryl urea derivatives possessing a 4H-pyrido[1,2-a]pyrimidin-4-one group as novel potent anticancer compounds. The structures were confirmed by IR,(1)H-NMR, and MS. All the compounds were screened for their antiproliferative activity against the human breast cancer cell line (MDA-MB-231). The pharmacological results indicated that most of the compounds showed moderate activity. The best of this series is compound 4c (IC(50)= 0.7 micromol/L), with a potency 3.6-fold higher than Sorafenib (IC(50) = 2.5 micromol/L), which was approved in 2005.
authors.affiliation: Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Ping Gong, 103 Wenhua Road, Shenyang, P. R. China.
authors.forename: Peng
authors.initials: P
authors.lastname: Yao
authors.forename: Xin
authors.initials: X
authors.lastname: Zhai
authors.forename: Dong
authors.initials: D
authors.lastname: Liu
authors.forename: Bao Hui
authors.initials: BH
authors.lastname: Qi
authors.forename: Hai Liang
authors.initials: HL
authors.lastname: Tan
authors.forename: Yong Cai
authors.initials: YC
authors.lastname: Jin
authors.forename: Ping
authors.initials: P
authors.lastname: Gong
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D011744:Pyrimidinones; D014508:Urea