Synthesis and bioactivity of 4,10-dimethyl-pyridino[2,3-h]quinolin-2(1H)-one-9-carboxylic acid and its esters |
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| 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 |
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| Institution: | Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 200032, China. |
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| 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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