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研究生:蔣宇東
論文名稱:合成1-基-3-乙醯胺及其相關化合物作為細胞分化劑
論文名稱(外文):Synthesis of 1-Benzyl Indole-3-acetamide and Related Compounds as Cell Differentiation Agent
指導教授:郭盛助 博 士黃麗嬌 博 士連金城 博 士
學位類別:碩士
校院名稱:中國醫藥學院
系所名稱:藥物化學研究所
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:2001
畢業學年度:89
語文別:中文
論文頁數:57
中文關鍵詞:基細胞分化劑
外文關鍵詞:BenzylIndoleCell Differentiation
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在持續尋找維甲酸對HL-60細胞之分化活性之增強劑中,著者合成了數個以-3-醋酸為先導化合物的類緣物。在測試這些標的化合物對於HL-60細胞的分化及增殖能力後,建立了初步的結構與活性關係。發現大部分的標的化合物能有效的加強維甲酸之作用。其中以化合物1-benzylindole-3-acetamide (4), N-methyl-1-
benzylindole-3-acetamide (5), N-ethyl-1-benzylindole-3-acetamide (6), N-n-propyl-1-benzylindole-3-acetamide (7),以及N-methyl-1-
benzylindole-3- carboxamide (13)具有最強的協同活性並選擇作進一步的評估。
As part of our continuing search for novel potentiators of the activity of retinoic acid in inducing differentiation of HL-60 cells, I have synthesized several analogs of the lead compound, indole-3-acetic acid. After testing the target compounds on HL-60 cells for differentiation and proliferation capability, a preliminary SAR was established.Most of the target compounds were found to be effective to potentiate the iuduction of different by retinoic acid.Among them, compound 1-benzylindole-3-
acetamide (4), N-methyl-1-benzylindole-3-acetamide (5), N-ethyl-1-
benzylindole-3-acetamide (6), N-n-propyl-1-benzylindole-3-acetamide (7),and N-methyl-1-benzylindole-3- carboxamide (13)showed most potent synesgistic activity and were selected for further evaluation.
中文摘要…………………………………………………………..1
英文摘要…………………………………………………………..2
第一章緒論………………………..……………………………3
第一節分化療法…………………………...………………3
第二節Retinoic acid (RA ) 臨床使用的現況...………………..5
第三節Indole-3-acetic acid (IAA) 在癌症治療上研究概況…….7
第二章研究動機與目的………………………...……………...9
第三章結果與討論………………………...………………….11
第一節化學合成………………………...…………………..11
第二節生物活性………………………...…………………..17
第四章結論………………………...………………………….23
第五章實驗部分………………………...…………………….24
第一節試藥………………………...……………………...24
第二節重要儀器與實驗材料……………………….…….26
第三節各化合物之製備………………………...………...28
第六章 參考文獻………………………...…………………….53重要圖譜
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