Fuyun Tian

Development of potent and selective ENPP1 inhibitors based on imidazo[1,2-a]pyrazine and pyrazine scaffolds for cancer immunotherapy.

In this study, new imidazo[1,2-a]pyrazine derivative 15 (YS3074) and pyrazine derivative 17 (YS3375) are identified and optimized as potent and selective ENPP1 inhibitors. Compounds 15 and 17 both exhibited high potency and selectivity toward ENPP1 (IC50 = 4.23 nM and 19.4 nM, respectively) with negligible ENPP2 inhibi...