SELENOLOPYRAZOLE類緣物之合成與生物活性（Ⅱ）

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Title:	SELENOLOPYRAZOLE類緣物之合成與生物活性（Ⅱ）
Authors:	郭盛助(Sheng-Chu Kuo);黃麗嬌(Li-Jiau Huang)
Contributors:	藥學院藥物化學研究所
Date:	2008-07-31
Issue Date:	2009-09-01 16:19:20 (UTC+8)
Abstract:	在我們不斷探索與開發新型的抗血小板與抗血管新生藥歷程中，曾經合成一系列indazole 類衍生物，並在這類雜環化合物中發現很多生物活性優異的物質。其中1-benzyl-3-(5』- hydroxymethyl-2』-furyl) indazole (YC-1)被証實是一種活性很強的血管新生抑制劑，具有開發潛能，可能成為治療癌症與血管新生相關疾病的藥物。在本計畫中，我們以selenolopyrazole 作為核心結構，將合成1, 3, 5-substituted selenolo [3, 2-c] pyrazole derivatives (I)及2, 3, 5-substituted selenolo [3, 2-c] pyrazole derivatives (II)等兩類衍生物。並評估這些標的化合物的抗血小板、抗心血管新生以及抗癌作用。我們預期在二年內找到數種新的先導化合物，進行這些先導化合物的優化並大量合成提供動物試驗。 In our continuing work aimed at the discovery and development of novel anti-platelet and anti-angiogenic agents, a series of indazole derivatives were synthesized, a lot of these compounds showed excellent biological activities. Among them, 1-benzyl-3-(5』-hydroxymethyl-2』-furyl) indazole (YC-1) was found to be a potent anti-angiogenesis inhibitor with the potential to become a useful agent in the treatment of human cancer and other angiogenesis-dependent diseases. In this research project, selenolopyrazole was selected as core structure, two series of 1,3,5-substituted selenolo [3,2-c] pyrazole derivatives (I) and 2,3,5-substituted selenolo [3,2-c] pyrazole derivatives (II), will be synthesized. The antiplatelet, antiangiogenesis and anticancer activities of these target compounds will be evaluated. We anticipate that the results in two-year period will lead to the identification of new lead compounds, the achievement of lead optimization and the accomplishment of large scale production of promising compounds for in vivo study.
Appears in Collections:	[Graduate Institute of Pharmaceutical Chemistry] Research reports

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