Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent

[Image: see text] Novel imidazole-based TGFβR1 inhibitors were identified and optimized for potency, selectivity, and pharmacokinetic and physicochemical characteristics. Herein, we report the discovery, optimization, and evaluation of a potent, selective, and orally bioavailable TGFβR1 inhibitor, 1...

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Wydane w:ACS Med Chem Lett
Główni autorzy: Velaparthi, Upender, Darne, Chetan Padmakar, Warrier, Jayakumar, Liu, Peiying, Rahaman, Hasibur, Augustine-Rauch, Karen, Parrish, Karen, Yang, Zheng, Swanson, Jesse, Brown, Jennifer, Dhar, Gopal, Anandam, Aravind, Holenarsipur, Vinay K., Palanisamy, Kamalavenkatesh, Wautlet, Barri S., Fereshteh, Mark P., Lippy, Jonathan, Tebben, Andrew J., Sheriff, Steven, Ruzanov, Max, Yan, Chunhong, Gupta, Anuradha, Gupta, Arun Kumar, Vetrichelvan, Muthalagu, Mathur, Arvind, Gelman, Marina, Singh, Rajinder, Kinsella, Todd, Murtaza, Anwar, Fargnoli, Joseph, Vite, Gregory, Borzilleri, Robert M.
Format: Artigo
Język:Inglês
Wydane: American Chemical Society 2020
Dostęp online:https://ncbi.nlm.nih.gov/pmc/articles/PMC7025382/
https://ncbi.nlm.nih.gov/pubmed/32071685
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00552
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