biostudies-literatureUnknown12(3)Zhang LIndoleamine 2,3-dioxygenase 1 (IDO1) has been identified as a target for small-molecule immunotherapy for the treatment of a variety of cancers including renal cell carcinoma and metastatic melanoma. This work focuses on the identification of IDO1 inhibitors containing replacements or isosteres for the amide found in BMS-986205, an amide-containing, IDO1-selective inhibitor currently in phase III clinical trials. Detailed subsequently are efforts to identify a structurally differentiated IDO1 inhibitor via the pursuit of a variety of heterocyclic isosteres, leading to the discovery of highly potent, imidazopyridine-containing IDO1 inhibitors.ACS medicinal chemistry letters494-501https://www.ebi.ac.uk/biostudies/studies/S-EPMC7958151biostudies-literatureDiscovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy.PMC7958151Balog AHuang CGullo-Brown JKopcho LBorzilleri RJohnston-Allegretto KPadmanabhan SZhang LDhar GMahankali SMurali VCherney ECLi XRajanna PMariappan TFereshteh MVite GLin TAAnandam AMaley DZhu XHunt JTTraeger SCfalseDiscovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy.Indoleamine 2,3-dioxygenase 1 (IDO1) has been identified as a target for small-molecule immunotherapy for the treatment of a variety of cancers including renal cell carcinoma and metastatic melanoma. This work focuses on the identification of IDO1 inhibitors containing replacements or isosteres for the amide found in BMS-986205, an amide-containing, IDO1-selective inhibitor currently in phase III clinical trials. Detailed subsequently are efforts to identify a structurally differentiated IDO1 inhibitor via the pursuit of a variety of heterocyclic isosteres, leading to the discovery of highly potent, imidazopyridine-containing IDO1 inhibitors.2021-01-01T00:00:00Z2021 Mar2025-04-19T12:53:47.851Z2025-04-19T12:53:47.851ZS-EPMC79581513373807710.1021/acsmedchemlett.1c00014