Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors

[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 inhi...

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Veröffentlicht in:ACS Med Chem Lett
Hauptverfasser: Su, Dai-Shi, Qu, Junya, Schulz, Mark, Blackledge, Chuck W., Yu, Hongyi, Zeng, Jenny, Burgess, Joelle, Reif, Alexander, Stern, Melissa, Nagarajan, Raman, Pappalardi, Melissa Baker, Wong, Kristen, Graves, Alan P., Bonnette, William, Wang, Liping, Elkins, Patricia, Knapp-Reed, Beth, Carson, Jeffrey D., McHugh, Charles, Mohammad, Helai, Kruger, Ryan, Luengo, Juan, Heerding, Dirk A., Creasy, Caretha L.
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2019
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7025381/
https://ncbi.nlm.nih.gov/pubmed/32071679
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00493
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