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

CMUR > College of Pharmacy > Graduate Institute of Pharmaceutical Chemistry > Proceedings > Item 310903500/22786

Please use this identifier to cite or link to this item: http://ir.cmu.edu.tw/ir/handle/310903500/22786

Title:	Synthesis and Cytotoxicity of the N2-Regioisomer Analogs of Ethyl 4-(1-benzyl-1H-indazol-3-yl)benzoate (YD-3)
Authors:	(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)
Contributors:	藥學院藥物化學研究所
Date:	2004-03-05
Issue Date:	2009-09-07 12:20:48 (UTC+8)
Abstract:	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.
Relation:	2004藥物化學研討會
Appears in Collections:	[Graduate Institute of Pharmaceutical Chemistry] Proceedings

Files in This Item:

There are no files associated with this item.