Challenges in the discovery of indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitors

…, SR Majjigapu, P Vogel, V Zoete…

Index: Roehrig, Ute F.; Majjigapu, Somi Reddy; Grosdidier, Aurelien; Bron, Sylvian; Stroobant, Vincent; Pilotte, Luc; Colau, Didier; Vogel, Pierre; Van Den Eynde, Benoit J.; Zoete, Vincent; Michielin, Olivier Journal of Medicinal Chemistry, 2012 , vol. 55, # 11 p. 5270 - 5290

Full Text: HTML

Citation Number: 20

Abstract

Since the discovery of indoleamine 2, 3-dioxygenase 1 (IDO1) as an attractive target for anticancer therapy in 2003, the search for inhibitors has been intensely pursued both in academia and in pharmaceutical companies. Many novel IDO1 inhibitor scaffolds have been described, and a few potent compounds have entered clinical trials. However, a significant number of the reported compounds contain problematic functional groups, suggesting that ...