設計合成phenylquinolone 類緣化合物做為抗癌藥

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 > 研究計畫 > Item 310903500/13391

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题名:	設計合成phenylquinolone 類緣化合物做為抗癌藥
作者:	郭盛助(Kuo,Sheng-Chu);黃麗嬌(Li-Jiau Huang);陳勝智(Sheng-Chih Chen);林宗平;連金城(Lien Jin Cherng);蔡尚元(Shang-Yuan Tsai);侯曼貞(Hour Mann-Jen)
贡献者:	藥學院藥物化學研究所
关键词:	前驅物;抗腫瘤活性;乳癌;Prodrug;Anti-tumor activity;Breast cancer;2-phenyl-4-quinolone;2-phenylnaphthyridin-4-one
日期:	2007-07-31
上传时间:	2009-09-01 16:20:54 (UTC+8)
摘要:	我們合成一系列substituted 2-phenyl-4-quinolones, 2-phenyl naphthyridin-4-ones及其prodrugs並從事其抗癌活性，結果發現CHM-2133P最為優越。我們以乳癌細胞MCF-7之 xenograftSCID mice model測試結果發現CHM-2133P，以劑量相關性的抑制腫瘤生長而且受試小鼠之體重並沒有明顯的變化。在本年度研究結果我們確認CHM- 2133P是一種頗具有開發潛能的新型抗有絲分裂抗癌藥，在體內、體外試驗都呈現對MCF-7乳癌細胞選擇性的強力抗腫瘤作用。 A series of substituted 2-phenyl-4- quinolones, 2-phenyl naphthyridin-4-ones and their prodrugs were synthesized and evaluated for their anti-cancer activities. Among them, CHM-2133P was the most promising agent. To investigate the in vivo anti-tumor activity of CHM-2133P, we carried out xenografts with MCF-7 cells in athymic SCID mice. CHM-2133P induced a dose-dependent inhibition of tumor growth. The body weights of treated animals were not significantly affected by CHM-2133P. In this study we identified that CHM- 2133P, as a potential novel anti-mitotic agent, which possess potent and selective anti-tumor activity against MCF-7 in vitro and in vivo tests.
显示于类别:	[藥物化學研究所] 研究計畫

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