4-苯胺呋喃[2,3-b]喹啉類衍生物之合成及生物活性的評估

Synthesis and Biological Evaluation of 4-Anilinofuro[2,3-b]quinoline Derivatives

梁治中(Chich-Chung Liung)

指導教授 ： 陳義龍

共同指導教授 ： 曾誠齊(Cherng-Chyi Tzeng)

高雄醫學大學/生命科學院/醫藥暨應用化學研究所/碩士(2007年)

摘要

最近我們發現4-anilinofuroquinoline衍生物如1-[4-(furo[2,3-b]quino
line-4-ylamino)-phenyl]ethanone (CIL-102) (GI50 = 0.025 M), 1-[4-(3-chloro-7-methoxyfuro[2,3-b]quinolin-4-ylamino)-phenyl]etha-
none 以及(CYL-698v)ethyl-4-(3-chloro-7-methoxyfuro[2,3-b]quinolin-
4-ylamino) benzoate (LHC-2608)具有抗癌的活性，這些化合物可以使細胞週期停滯在G2/M期，它們的抗癌機制是影響微小管的聚合作用而使有絲分裂失敗，造成細胞凋亡。根據structure-activity relationships的結果，為了增進這些化合物的抗癌活性，我們合成出一系列在furo[2,3-b]quinoline的4-C位置上具有anilines取代的衍生物，在本篇論文中所合成出的新衍生物，並沒有發現比CIL-102活性表現更優良的衍生物。

關鍵字

呋喃喹啉

並列摘要

Recently, we have found certain 4-anilinofuroquinoline derivatives such as 1-[4-(furo[2,3-b]quinolin-4-ylamino)-phenyl]ethanone (CIL-102) (GI50 = 0.025 M) and 1-[4-(3-chloro-7-methoxyfuro[2,3-b]quinolin-4-ylamino)
-phenyl]ethanone (CYL-698v) and ethyl-4-(3-chloro-7-methoxyfuro
[2,3-b]quinolin-4-ylamino)benzoate (LHC-2608) to possess potent anticancer activities. These compounds arrest the cell cycle in G2/M phase. Further pharmacological evaluation revealed that these 4-anilino-
furoquinolines interact with microtubule polymerization and causes mi-
totic arrest followed by apoptosis. To optimize anticancer activities and
to establish structure-activity relationships, we have synthesized a number of new entities with various substituents at 4-C position of 4-anilino moiety for antiproliferative evaluation. None of the newly syn-
thesized 4-anilinofuroquinoline derivatives proved to be more potent than that of CIL-102 。

並列關鍵字

furo quinoline

參考文獻

參考資料

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