Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors

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 op...

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Veröffentlicht in:	ACS medicinal chemistry letters 2020-02, Vol.11 (2), p.133-140
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:	Artikel
Sprache:	eng
Schlagworte:	Letter
Online-Zugang:	Volltext
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