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Development of a series of novel o-phenylenediamine-based indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors |
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| Authors: | David K. Williams Jay A. Markwalder Aaron J. Balog Bin Chen Libing Chen Jennifer Donnell Lauren Haque Amy C. Hart Sunil K. Mandal Andrew Nation Weifang Shan Gregory D. Vite Kelly Covello John T. Hunt Maria N. Jure-Kunkel Steven P. Seitz |
| Affiliation: | 1. Oncology Chemistry, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States;2. Biocon BMS Research and Development Center (BBRC), Syngene International Ltd, Plat No. 2 & 3, Bommasandra IV Phase, Jigani Link Road, Bangalore 560 099, India;3. MedImmune, One MedImmune Way, Gaithersburg, MD 020874, United States;4. Oncology Biology, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States |
| Abstract: | A novel series of o-phenylenediamine-based inhibitors of indoleamine 2,3-dioxygenase (IDO) has been identified. IDO is a heme-containing enzyme, overexpressed in the tumor microenvironment of many cancers, which can contribute to the suppression of the host immune system. Synthetic modifications to a previously described diarylether series resulted in an additional degree of molecular diversity which was exploited to afford compounds that demonstrated significant potency in the HeLa human cervical cancer IDO1 assay.. |
| Keywords: | Indoleamine 2,3-dioxygenase IDO IDO1 Immuno-oncology Kynurenine |
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