(E)-4-苯胺-2-苯乙烯喹啉衍生物之合成及生物活性的評估

Synthesis and Biological Evaluation of Certain (E)-4-Anilino-2-styrylquinoline Derivatives

林錫峻(Shi-Jiun Lin)

指導教授 ： 曾誠齊

高雄醫學大學/生命科學院/醫藥暨應用化學研究所碩士在職專班/碩士(2008年)

摘要

很多天然與合成的抗癌試藥都已經被發現具有2-phenylnaphthalene的骨架。例如2-phenylquinoline-8-carboxamide 的衍生物顯示出具有DNA-binding之能力以及對白血病和固體腫瘤生物活性分析有廣效的活性。在我們研究團隊中4-anilino-2-phenylquinolone的衍生物也證實有不錯的抗癌活性。為了發展更有潛力的抗癌試劑和建立完整的結構與活性的關係，因此我們合成出類似2-phenylnaphthalene架構及結合上共振雙鍵架橋的具有抗增生活性之4-anilino-2-styrylquinoline衍生物。同時，我們也合成出含有oxime和methyloxime的衍生物來測試 活性。在這些合成的化合物中以11、14a、15a和15b具有很明顯的抗細胞增生活性。

關鍵字

苯乙烯喹啉苯胺

並列摘要

A large number of natural and synthetic anticancer agents have been found to possess the 2-phenylnaphthalene skeleton. For example, 2-phenyl quinoline-8-carboxamide derivatives have been shown to possess DNA-binding capability and broad-spectrum activities in both leukemia and solid-tumor assays. Certain 4-anilino-2-phenylquinolone derivatives were also proved to possess potent anticancer activities by our research group. To explore more potent anticancer agents and establish structure-activity relationships, we described herein the preparation and antiproliferative activities of certain 4-anilino-2-styrylquinoline derivatives whose structures belong to the common structural pattern of 2-phenylnaphthalene with an additional conjugated double bond bridge. Their oxime and methyloxime derivatives were also synthesized for evaluation. Among them, compounds 11, 14a, 15a, and 15b exhibited significant antiproliferative activities.

並列關鍵字

styrylquinoline ； Anilino

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