Discovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy
| Autor: | Mark Fereshteh, Xiao Zhu, Tai-An Lin, Prabhakar Rajanna, Cherney Emily Charlotte, Aravind Anandam, Xin Li, Derrick Maley, Liping Zhang, Gopal Dhar, Aaron Balog, Robert M. Borzilleri, Johnni Gullo-Brown, T. Thanga Mariappan, Kathy Johnston-Allegretto, Christine Huang, Venkata Murali, John T. Hunt, Sandeep Mahankali, Gregory D. Vite, Lisa M. Kopcho, Shweta Padmanabhan, Sarah C. Traeger |
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| Rok vydání: | 2021 |
| Předmět: |
Metastatic melanoma
010405 organic chemistry business.industry medicine.medical_treatment Organic Chemistry Phases of clinical research Immunotherapy medicine.disease 01 natural sciences Biochemistry 0104 chemical sciences 010404 medicinal & biomolecular chemistry Cancer immunotherapy Renal cell carcinoma Drug Discovery medicine Cancer research business Indoleamine 2 3-dioxygenase |
| Zdroj: | ACS Med Chem Lett |
| ISSN: | 1948-5875 |
| DOI: | 10.1021/acsmedchemlett.1c00014 |
| Popis: | [Image: see text] 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. |
| Databáze: | OpenAIRE |
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