2–苯基–4-喹啉酮-3–羧酸衍生物之合成及抗癌活性; Synthesis and anti-cancer activity of 2–phenyl-4-quinolone-3-carboxylic acid derivatives

中國醫藥大學機構典藏 China Medical University Repository, Taiwan > 藥學院 > 藥物化學研究所 > 博碩士論文 > Item 310903500/923

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题名:	2–苯基–4-喹啉酮-3–羧酸衍生物之合成及抗癌活性;Synthesis and anti-cancer activity of 2–phenyl-4-quinolone-3-carboxylic acid derivatives
作者:	莊仕弘;Shi-Hong Zshuang
贡献者:	中國醫藥大學：藥物化學研究所碩士班
关键词:	抗癌活性;2–苯基–4–喹;啉;酮-3–羧酸;anti-cancer activity;2–phenyl-4-quinolone-3-carboxylic acid;2-PQ
日期:	2007-07-10
上传时间:	2009-08-13 09:37:20 (UTC+8)
摘要:	在我們不斷的探索及開發新穎抗癌藥的歷程中，2-(3-fluorophenyl)-6-methoxy-4-quinolone-3-carboxylic acid被發現為具有良好抗癌活性的候選藥物。由於此項初步成果，因而以2-(3-fluorophenyl)-6-methoxy-4-quinolone-3-carboxylic acid為先導化合物，合成一系列2-(2,3- substituted phenyl)-6,7-substituted 4-quinolone-3-methanols (42–55)、2-(2,3-substituted phenyl)-6,7-substituted 4-quinolone-3-carbaldehydes (56–58)、2-(2,3-substituted phenyl)-6,7-substituted 4-quinolone-3-oximes (59–64)、及2-(2,3-substituted phenyl)-N-substituted-6,7-substituted 4- quinolone-carboxamides (65–94)的化合物。檢視標的化合物的42–94 的細胞致毒活性及aurora A kinase 抑制活性。初步結果顯示化合物3-((2-Hydroxyethylimino)methyl) -6-methoxy-2-phenyl-4-quinolone (61)以及3-((2-Hydroxyethylimino) methyl)-6,7-methylenedioxy-2-phenyl-4-quinolone (62)具有明顯的aurora A kinase抑制活性，二者值得更深入的探討。 In our continuing work aimed at the discovery and development of novel anticancer agents, 2-(3-fluorophenyl)-6-methoxy-4-quinolone-3- carboxylic acid was identified as a promising anticancer drug candidate. Encouraged by the preliminary results, 2-(3-fluorophenyl)-6- methoxy-4-quinolone-3-carboxylic acid was used as a lead compound, a series of 2-(2,3-substituted phenyl)-6,7-substituted 4-quinolone-3- methanols (42 – 55), 2-(2,3-substituted phenyl)-6,7-substituted 4-quinolone-3-carbaldehydes (56–58), 2-(2,3-substituted phenyl)-6, 7-substituted 4-quinolone-3-oximes (59–64), and 2-(2,3-substituted phenyl) -N-substituted-6, 7-substituted 4-quinolone-carboxamides (65–94) were synthesized. The target compound 42–94 were examined for their cytotoxicity and inhibitory effect on aurora A kinase activity. Preliminary results showed that 3-((2-hydroxyethylimino)methyl)-6-methoxy-2-phenyl-4- quinolone (61) and 3-((2-hydroxyethylimino)methyl)-6,7-methylenedioxy -2-phenyl-4-quinolone (62) exhibited significant effect on aurora A kinase. These two compounds are worthy for further exploration.
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