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研究生:黃雅蘋
研究生(外文):Ya-Ping Huang
論文名稱:取代之喹唑啉類衍生物的合成以及抗增生活性評估
論文名稱(外文):Synthesis and Antiproliferative Evaluation of Substituted Quinazoline Derivatives
指導教授:陳義龍
指導教授(外文):Yeh-Long Chen
學位類別:碩士
校院名稱:高雄醫學大學
系所名稱:醫藥暨應用化學研究所
學門:醫藥衛生學門
學類:藥學學類
論文種類:學術論文
論文出版年:2012
畢業學年度:100
語文別:中文
論文頁數:110
中文關鍵詞:唑啉唑啉唑啉唑啉
外文關鍵詞:4-substituted and 2-substituted-vinyl quinazoline derivativesantiproliferatve activities
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喹唑啉類的衍生物在很多文獻中被發現具有很多不錯的生物活性,本研究主要合成一系列喹唑啉2位及4位不同取代基的化合物。

我們合成在2位及4位上不同取代的喹唑啉的衍生物,並在C-4的位置具有不同官能基的取代,並進行抗增生活性的評估。結果顯示這些化合物對於肺癌細胞 (H460、H1299)、乳癌細胞 (MB231) 等常見的人類癌細胞株具有很強的抗癌活性, 當中4-苯胺-2-硝基呋喃為最強抑制癌細胞株的化合物。


Quinazoline derivatives have been found to possess a wide variety of biological activities. The aims of this thesis are to synthesize and evaluate a series of 4-substituted and 2-substituted-vinyl quinazoline derivatives. These 4-substituted and 2-substituted-vinyl quinazoline derivatives with various substituents at the C-4 position of quinazoline skeleton and at the vinyl moiety have been synthesized and evaluated for their antiproliferatve activities. Results indicated that most of these newly synthesized compounds exhibited potent activities against the growth of all the cancer cells tested including lung cancer cells (H460, H1299) and breast cancer cells (MB231) in which 4-anilino-2-(5-nitrofuran-2-yl)- vinyl quinazoline derivatives have been found to be the most potent in the growth inhibition of these cancer cell lines.

中文摘要---------------------------------------------------------------------- 1
英文摘要---------------------------------------------------------------------- 2
壹、 緒論--------------------------------------------------------------------- 3
貳、 研究動機--------------------------------------------------------------- 7
參、 合成方法、結果與討論
第一部分 ----------------------------------------------------------------------- 18
一、4-Anilino-2-furanylvinylquinazoline quinazoline骨架逆合成分析 二、4-Anilino-2-furanylvinylquinazoline衍生物逆合成分析
三、4-Anilino-2-furanylvinylquinazoline衍生物的合成
四、Oxime 側鏈的合成
第二部分 ----------------------------------------------------------------------- 34
一、8-hydroxy-2-substituted quinoline衍生物的合成
二、2- substituted quinazolinone 衍生物的合成
三、4-Anilino-2- substituted quinazoline 衍生物的合成
肆、 生物活性結果與討論
第一部分 ----------------------------------------------------------------------- 29
第二部分 ----------------------------------------------------------------------- 37
伍、結論 --------------------------------------------------------------------- 41
陸、實驗部分 --------------------------------------------------------------- 42
柒、參考文獻 --------------------------------------------------------------- 104 附錄 ---------------------------------------------------------------------------- 108


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