Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model
A hydroxyamidine chemotype has been discovered as a key pharmacophore in novel inhibitors of indoleamine 2,3-dioxygenase (IDO). Optimization led to the identification of 5l, which is a potent (HeLa IC50=19 nM) competitive inhibitor of IDO. Testing of 5l i
Yue, Eddy W.,Douty, Brent,Wayland, Brian,Bower, Michael,Liu, Xiangdong,Leffet, Lynn,Wang, Qian,Bowman, Kevin J.,Hansbury, Michael J.,Liu, Changnian,Wei, Min,Li, Yanlong,Wynn, Richard,Burn, Timothy C.,Koblish, Holly K.,Fridman, Jordan S.,Metcalf, Brian,Scherle, Peggy A.,Combs, Andrew P.
supporting information; experimental part
p. 7364 - 7367
(2010/06/11)
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