| Autor: |
Ryan G. Kruger, Junya Qu, Dai-Shi Su, Helai P. Mohammad, Melissa B. Pappalardi, Patricia A. Elkins, Alan P. Graves, Dirk A. Heerding, William G. Bonnette, Joelle Lorraine Burgess, Juan I. Luengo, Jenny Zeng, Beth Anne Knapp-Reed, Mark J. Schulz, Alexander Joseph Reif, Jeffrey D. Carson, Raman P. Nagarajan, Caretha L. Creasy, Chuck W Blackledge, Kristen Wong, Melissa Stern, Charles F. McHugh, Hongyi Yu, Liping Wang |
| Rok vydání: |
2019 |
| Předmět: |
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| Zdroj: |
ACS Med Chem Lett |
| ISSN: |
1948-5875 |
| Popis: |
[Image: see text] We report herein the discovery of isoxazole amides as potent and selective SET and MYND Domain-Containing Protein 3 (SMYD3) inhibitors. Elucidation of the structure–activity relationship of the high-throughput screening (HTS) lead compound 1 provided potent and selective SMYD3 inhibitors. The SAR optimization, cocrystal structures of small molecules with SMYD3, and mode of inhibition (MOI) characterization of compounds are described. The synthesis and biological and pharmacokinetic profiles of compounds are also presented. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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