臺灣博碩士論文加值系統

本研究主要探討具有DNA嵌入劑結構特徵之茚[1,2-b]喹啉類衍生物的合成與抗腫瘤活性的評估。研究結果發現，細胞毒殺活性主要取決於茚[1,2-b]喹啉的平面骨架與環上所導入的鹼性側鏈。而環上的10號與11號位置是決定抗增生活性關鍵位置，其中具有aminoalkoxyimino取代之10-methyl-11H-indeno[1,2-b]quinolin-11-one O-aminoalkyl oxime (8c-h)，11-oxo-11H-indeno[1,2-b]quinoline-10-carbaldehyde O-aminoalkyl oxime (14d-j)，11H-indeno[1,2-b]quino-line-10-carbaldehyde O-aminoalkyl oxime (20a-e)，衍生物有非常顯著的抗腫瘤活性，在4 μg/mL的濃度時能幾乎100% 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-indeno[1,2-b]quinoline derivatives with the structural characteristics of DNA intercalator are described. The results of this study indicate that the cytotoxic effect depends on the basic side chains that substituted in the planar nucleus of 11H-indeno[1,2-b]quinoline. Substituents at C-10 and C-11 positions are crucial to the antiproliferative potency of 11H-indeno[1,2-b]quinoline, the aminoalkoxyimino substitutent of10-methyl-11H-indeno[1,2-b]quinolin-11-one (8c-h), 11-oxo-11H-indeno[1,2-b]quinoline-10-carbaldhyde (14d-j),11H-indeno[1,2-b]quinoline-10-carbaldehyde derivatives (20a-e), 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 ----------------------------------------------------3
貳、研究動機 ------------------------------------------------13
參、研究方法 ------------------------------------------------19
肆、合成結果與討論
一、11-取代茚[1,2-b]喹啉衍生物之合成 ------------------------22
二、alkoxyamines 之合成 ------------------------------------24
三、10-取代茚[1,2-b]喹啉-11-酮衍生物之合成 -------------------26
四、10-取代茚[1,2-b]喹啉衍生物之合成 ------------------------29
伍、抗癌活性結果討論
一、11-取代茚[1,2-b]喹啉衍生物之體外癌細胞抑制能力百分比 ------33
二、10-取代茚[1,2-b]喹啉-11-酮衍生物體外癌細胞抑制能力百分比---36
三、10-取代茚[1,2-b]喹啉衍生物之體外癌細胞抑制能力百分比 ------38
陸、結論 ----------------------------------------------------39
柒、實驗部分
一、溶劑及處理過程 ---------------------------------------40
二、儀器 -------------------------------------------------40
三、試藥 -------------------------------------------------41
四、化合物製備過程 ---------------------------------------44
五、抗癌活性實驗 -----------------------------------------84
捌、參考文獻 ------------------------------------------------86
附錄 -------------------------------------------------------92

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