Discovery of Imidazopyridines as Potent Inhibitors
of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy |
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| Authors: | Liping Zhang Emily C Cherney Xiao Zhu Tai-an Lin Johnni Gullo-Brown Derrick Maley Kathy Johnston-Allegretto Lisa Kopcho Mark Fereshteh Christine Huang Xin Li Sarah C Traeger Gopal Dhar Aravind Anandam Sandeep Mahankali Shweta Padmanabhan Prabhakar Rajanna Venkata Murali Thanga Mariappan Robert Borzilleri Gregory Vite John T Hunt Aaron Balog |
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| Institution: | †Bristol Myers Squibb Research and Development, Princeton, New Jersey 08543-4000, United States;‡Biocon Bristol Myers Squibb R&D Center, Biocon Park, Jigani Link Road, Bengaluru, Karnataka 560099, India |
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| Abstract: | 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. |
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| Keywords: | Indoleamine 2 3-dioxygenase 1 IDO1 immuno-oncology amide isostere |
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