title: Synthesis and bioactivity of 4,10-dimethyl-pyridino[2,3-h]quinolin-2(1H)-one-9-carboxylic acid and its esters.
abstract: 4,10-Dimethyl-pyridino[2,3-h]quinolin-2(1H)-one-9-carboxylic acid (1) was synthesized by a new approach via the key intermediate 7-[1-aza-2-(dimethylamino)vinyl]-4-methylquinolin-2(1H)-one (4). Compound 1 and its esters were evaluated in cytotoxicity and anti-HIV assays. The 9-carboxyl (1s)-endo-(-)-borneol ester (9) showed marginal cytotoxic activity in CAK1-1, HOS, KB, and HCT-8 cells.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 200032, China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Zhang
authors.forename: Ying
authors.initials: Y
authors.lastname: Chen
authors.forename: Yun Qing
authors.initials: YQ
authors.lastname: Zheng
authors.forename: Peng
authors.initials: P
authors.lastname: Xia
authors.forename: Yi
authors.initials: Y
authors.lastname: Xia
authors.forename: Zheng Yu
authors.initials: ZY
authors.lastname: Yang
authors.forename: Kenneth F
authors.initials: KF
authors.lastname: Bastow
authors.forename: Susan L
authors.initials: SL
authors.lastname: Morris-Natschke
authors.forename: Kuo Hsiung
authors.initials: KH
authors.lastname: Lee
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D004354:Drug Screening Assays, Antitumor; D006678:HIV / Q000187:drug effects; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: C478827:4,10-dimethyl-pyridino(2,3-h)quinolin-2(1H)-one-9-carboxylic acid; D019380:Anti-HIV Agents; D000970:Antineoplastic Agents; D007202:Indicators and Reagents; D015363:Quinolones