臺灣博碩士論文加值系統

中文摘要
本研究合成一系列具有嵌入DNA而抑制TopoⅡ潛能之Benzo[4,5]furo[3,2-b]-quinoline衍生物，並導入各種不同胺類取代之側鏈。這些化合物正在美國National Cancer Institute測試六十種人類癌細胞活性，包括白血病、小型肺細胞癌、肺癌、中樞神經系統癌、黑色素瘤、卵巢癌、腎臟癌、前列腺癌和乳癌等九大類癌細胞1之抗癌活性評估，希望能藉著構造與活性關係之探討尋找具有抗癌潛力之新化合物。

Abstract
Intercalation with DNA to lead inhibition of mammadian topoisomerase II is known to occur for compounds possessing coplanar aromatic chromophores. The noticeable examples of DNA-intercalating agents are adriamycin, actinomycin, ellipticine, amsacrine and mitoxantrone which have been widely used for the treatment of cancer patients.
The present research project is aimed at the synthesis and evaluation of certain tetracyclic benzofuro [3,2-b] quinoline derivatives in which an additional aromatic ring is linearly fused on the potential anticancer furoquinoline. The same strategy had been proved to be successful in which acronycine analogue, with an additional aromatic ring linearly fused on its A-ring to enhance DNA-intercalating capability, exhibited ten-fold more potent than the parent acronycine in inhibiting L1210 cell proliferatin. The advantages of these compounds are to maintain a coplanar tetracyclic DNA-intercalating chromophores and improve their DNA-intercalating capability. Their substituted derivatives have also been synthesized and evaluated for anticancer activities.

目錄
中文摘要
英文摘要
壹、緒言
貳、研究動機
參、合成方式、結果及討論
一、 平面直線四環(6.6.5.6)合成方法、結果及討論
二、 脂肪族胺取代之合成、結果及討論
三、 芳香胺取代之合成、結果及討論
肆、藥理活性測試實驗方法與活性結果探討
一、實驗方式
二、結果探討
伍、實驗部分
一、 試藥
二、 裝置
三、 儀器
四、 各化合物製備
陸、參考文獻
柒、產物碳、氫核磁共振光譜

陸、參考文獻
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