臺灣博碩士論文加值系統

本研究主要探討具有DNA嵌入劑結構特徵之11H-indolo[3,2-c]quinoline類衍生物的合成與抗腫瘤活性的評估。11H-indolo[3,2-c]quinoline 是藉由氮原子將2-phenylnaphthalene 結合成共平面四環的多融合雜環芳香化合物，部分的化合物且已被證實為DNA 嵌入劑並具有抗增生活性。本文研究結果發現，細胞毒殺活性主要取決於平面架構的11H-indolo[3,2-c]quinoline環上所導入的鹼性側鏈。其中具有O-alkyloximes取代之indoloquinoline衍生物 (3e, 3f, 3g, 5c)有非常顯著的抗腫瘤活性，在4 μg/mL的濃度時能幾乎95% 抑制MCF-7 (乳癌細胞)，NCI-H460 (肺癌細胞)，SF-268 (中樞神經癌細胞)的生長。

Synthesis and antiproliferative evaluation of 11H-indolo[3,2-c]quinoline derivatives with the structural characteristics of DNA-intercalator are described. 11H-Indolo[3,2-c]quinoline is a coplanar tetracyclic heterocycle in which the consisting 2-phenyl- naphthalene are conformationally locked through a nitrogen bridge. The results of this study indicate that the cytotoxic effect depends on the basic side chains inserted in the planar nucleus of 11H-indolo[3,2-c]quinoline. The O-alkyloximes substituted of indoloquinoline derivatives(3e, 3f, 3g, 5c), which show the most significant antiproliferative activity on the growth of MCF-7, NCI-H460, and SF-268 at a concentration of 4 μg/mL.

目錄
中文摘要 ---------------------------------------1
英文摘要 ---------------------------------------2
壹、緒言
一、前言 -----------------------------------3
二、研究動機 -------------------------------7
貳、實驗方法------------------------------------14
參、實驗結果與討論 -----------------------------17
肆、藥理活性測試實驗方法與活性結果討論
一、實驗方式 -------------------------------27
二、活性結果與討論 -------------------------29
三、結論 -----------------------------------31
伍、實驗部分
一、溶劑及處理過程 -------------------------32
二、儀器及試藥 -----------------------------33
三、各化合物製備過程 -----------------------36
陸、參考文獻 -----------------------------------64

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