Synthesis and Cytotoxicity of the N2-Regioisomer Analogs of Ethyl 4-(1-benzyl-1H-indazol-3-yl)benzoate (YD-3)

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題名:	Synthesis and Cytotoxicity of the N2-Regioisomer Analogs of Ethyl 4-(1-benzyl-1H-indazol-3-yl)benzoate (YD-3)
作者:	(Hua-Sin Chen);林鈺富(Yu-Fu Lin);(Chun-Jen Chen ();(Yi-Chien Lin);(Jing-Je Huang ();(Shi-Hong Zhuang);黃麗嬌(Li-Jiau Huang);郭盛助(Sheng-Chu Kuo)
貢獻者:	藥學院藥物化學研究所
日期:	2004-03-05
上傳時間:	2009-09-07 12:20:48 (UTC+8)
摘要:	Ethyl 4-(1-benzyl-1H-indazol-3-yl)benzoate (YD-3) was first synthesized in our laboratory as a novel inhibitor of protease-activated receptor 4 (PAR4) in platelet. In this study, a series of N2-regioisomer analogs (5—10) of YD-3 was synthesized and examined for their cytotoxicity. The starting material, 1-(N-morpholino)cyclohexene, was treated with terephthalic acid monomethyl ester chloride via a Stork enamine reaction to yield methyl 4-[(2-oxocyclohexyl)carbonyl]benzoate (1). Compound 1 was treated with hydrazine hydrate to yield methyl 4-(4,5,6,7-tetrahydro-1H-indazol-3-yl)benzoate (2). Subsequently, compound 2 was treated with palladium and the mixture was heated to form the expected 3 with high yield. Starting from 3, various N2-regioisomer analogs (5—10) of YD-3 were synthesized. These N2-regioisomer analogs (5—10) of YD-3 were assayed for their cytotoxicity against HL-60, A549 and HA22T cell lines. Among them, compounds 2 and 10 showed significant cytotoxicity.
關聯:	2004藥物化學研討會
顯示於類別:	[藥物化學研究所] 會議論文

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