title: Synthesis and in vitro antiproliferative evaluation of pyrimido[5,4-c]quinoline-4-(3H)-one derivatives.
abstract: A series of pyrimido[5,4-c]quinoline-4-(3H)-one derivatives variously substituted at positions 2 and 3 were synthesized and evaluated for their in vitro antiproliferative activities against a panel of six human cancer cell lines. Biological evaluation revealed that the vast majority of derivatives exhibited moderate tumor growth inhibitory activities. In particular, compound 7e showed effective anti-tumor activity with broad-spectrum toward numerous cell lines and the most active member in this study. This derivative displaying significant activity against KB (IC(50): 4.9 μM), CNE2 (IC(50): 13.8 μM), MGC-803 (IC(50): 4.8 μM), GLC-82 (IC(50): 7.88 μM), MDA-MB-453 (IC(50): 18.2 μM) and MCF-7 (IC(50): 10.1 μM) cell lines could be considered as the most promising and useful template for future development to obtain more potent anti-tumor agent(s).
authors.affiliation: Laboratory for Natural Product Chemistry, College of Pharmacy, South Central University for Nationalities, 708 Minyuan Road, Wuhan 430074, PR China.
authors.forename: Yong
authors.initials: Y
authors.lastname: Ai
authors.forename: Yong-Ju
authors.initials: YJ
authors.lastname: Liang
authors.forename: Jian-Chao
authors.initials: JC
authors.lastname: Liu
authors.forename: Hong-Wu
authors.initials: HW
authors.lastname: He
authors.forename: Yu
authors.initials: Y
authors.lastname: Chen
authors.forename: Chu
authors.initials: C
authors.lastname: Tang
authors.forename: Guang-Zhong
authors.initials: GZ
authors.lastname: Yang
authors.forename: Li-Wu
authors.initials: LW
authors.lastname: Fu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D015363:Quinolones