2-(3-Fluorophenyl)-6-Methoxy-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid衍生物之合成與抗癌活性

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题名:	2-(3-Fluorophenyl)-6-Methoxy-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid衍生物之合成與抗癌活性
其它题名:	Synthesis and Anticancer Activity of 2-(3-Fluorophenyl)-6-Methoxy-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid Derivatives
作者:	黃麗嬌(Li-Jiau Huang)
贡献者:	藥學院藥物化學研究所
日期:	2008-07-31
上传时间:	2009-09-01 16:19:26 (UTC+8)
摘要:	本研究室過去合成了一系列3』，6-substituted 2-phenyl-4-quinolone-3- carboxylic acid 衍生物，經抗癌活性評估結果，以化合物2-(3-fluorophenyl)-6- methoxyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (D-1)之活性最佳，被認為是個良好的先導化合物，值得進一步開發。在本計畫中，我們將以D-1 為先導化合物，從事其類緣物I、II、III 及IV 等類之合成，並將評估標的化合物之細胞致毒、作用機轉及抗腫瘤活性，期待能建立各類化合物之結構與活性關係，並進行先導化合物之最適化。 In our previous work, 3』, 6-substituted 2-phenyl-4-quinolone-3-carboxylic acid derivatives were synthesized and evaluated for their anticancer activity. Among these tested compounds, 2-(3-fluorophenyl)-6-methoxyl-4-oxo-1,4-dihydroquinoline-3- carboxylic acid (D-1) was the most promising one which was identified as an excellent lead compound and worthy for further investigation. In the present work, D-1 was selected as lead compound, several analogs including I, II, III and IV will be synthesized, The cytotoxicity, action mechanism and antitumor activity of these target compounds will be evaluated. We hope to establish the structure-activity relationships of these compounds and achieve optimization of lead compound D-1.
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