Structure–activity relationship and enzyme kinetic studies on 4-aryl-1H-1, 2, 3-triazoles as indoleamine 2, 3-dioxygenase (IDO) inhibitors

Q Huang, M Zheng, S Yang, C Kuang, C Yu…

Index: Huang, Qiang; Zheng, Maofa; Yang, Shuangshuang; Kuang, Chunxiang; Yu, Cunjing; Yang, Qing European Journal of Medicinal Chemistry, 2011 , vol. 46, # 11 p. 5680 - 5687

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Citation Number: 25

Abstract

Previously, we have reported the design and synthesis of 4-aryl-1H-1, 2, 3-triazoles as inhibitors of indoleamine 2, 3-dioxygenase (IDO), a promising therapeutic target of cancer. Here, we present the structure–activity relationship and enzyme kinetic studies on a series of 4-aryl-1H-1, 2, 3-triazoles. Three compounds (1, 6, 8) were found to possess more IDO inhibitory potency than the most commonly used 1-methyltryptophan. The results from the ...