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 ...