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研究生:黃尊遠
研究生(外文):Zun-Yuan Huang
論文名稱:4-苯胺呋喃[2,3-b]喹啉和苯乙烯基喹啉類衍生物之合成及生物活性的評估
論文名稱(外文):Synthesis and Biological Evaluationof 4-Anilinofuro[2,3-b]quinoline andStyrylquinoline Derivatives
指導教授:陳義龍
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碩士班
學門:生命科學學門
學類:生物科技學類
論文種類:學術論文
論文出版年:2006
畢業學年度:94
語文別:中文
論文頁數:185
中文關鍵詞:
外文關鍵詞:quinoline
相關次數:
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2-苯基萘骨架結構的喹啉酮類抗腫瘤的藥劑,被Lee等研究人員發現它是一種抑制有絲分裂的抗腫瘤試劑與管細胞相互作用。我們實驗室所合成的2-苯基-8-羥基喹啉衍生物有蠻不錯的抑制細胞增生活性,而類似物苯乙烯基喹啉類已被發現具有抗HIV-1的生物活性,因此我們合成出一系列苯乙烯基喹啉類衍生物並探討其抗癌的生物活性,並發現化合物27,35具有良好的抑制細胞增生活性。
而從芸香科植物中萃取出呋喃喹啉之生物鹼具有抗癌、抗菌、抗濾過性病毒等生物活性。我們實驗室所合成的4-苯胺呋喃[2,3-b]喹啉衍生物也有良好抑制細胞增生的活性,這一系列藥物也被報導他們的作用機制與2-苯基萘骨架結構的喹啉酮類抗腫瘤的藥劑是相同的,因此我們想以4-苯胺呋喃[2,3-b]喹啉為主架構,並在苯胺的3號碳上增加側鏈,希望能提高它的血液中溶解度。
2-phenyl-4-quinolone derivatives have been found as anti-tumor agents and Lee etc found their to interacted with tubuline and caused mitotic arrest. We synthesized certain 2-phenyl-8-hydroxyquinoline derivatives to have potent proliferativty. Us analyse styrylquinoline have been reported to have various biological activities such as anti-HIV1. Therefore, we synthesized styrylquinoline derivatives and evaluted their anticancer activities. We found that Compounds 27,35 have potent proliferativty.
The furoquinoline alkaloids isolated from the Rutaceac family of plants have various biological activities such as anticancer, antibacterial and antiviral effects. We synthesized certain 4-anilinofuro[2,3-b] quinoline derivatives and some compounds have potent proliferativty.These compounds haved the same mechanism as the 2-phenyl-4-quinolones.We order to improve free in serum. Therefore.We synthesized used derivative of 4-anilinofuro[2,3-b]quinoline by additing the side chain at C3.
目錄
中文摘要 ---------------------------------------6
英文摘要 ---------------------------------------7
壹、緒言
一、癌症的簡介------------------------------9
二、細胞週期與癌症的關係--------------------10
貳、研究動機------------------------------------13
参、合成的方式、結果與討論
一、Styrylquinoline衍生物之結果與討論---------22
二、逆合成分析------------------------------25
三、呋喃喹啉類衍生物合成--------------------26
肆、藥理活性測試實驗方法與活性結果討論
一、實驗方式 -------------------------------34
二、活性結果與討論 -------------------------35
伍、實驗部分
一、溶劑及處理過程 -------------------------39
二、儀器及試藥 -----------------------------41
三、各化合物的製備 -------------------------43
陸、參考文獻 -----------------------------------92
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