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Synthesis and bioactivity of 4,10-dimethyl-pyridino[2,3-h]quinolin-2(1H)-one-9-carboxylic acid and its esters
Authors:Zhang Qian  Chen Ying  Zheng Yun Qing  Xia Peng  Xia Yi  Yang Zheng Yu  Bastow Kenneth F  Morris-Natschke Susan L  Lee Kuo Hsiung
Institution:Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 200032, China.
Abstract:4,10-Dimethyl-pyridino2,3-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.
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