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Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2019 Dec 27; Vol. 11 (2), pp. 133-140. Date of Electronic Publication: 2019 Dec 27 (Print Publication: 2020). - Publication Year :
- 2019
-
Abstract
- 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.<br />Competing Interests: The authors declare no competing financial interest.<br /> (Copyright © 2019 American Chemical Society.)
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 11
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 32071679
- Full Text :
- https://doi.org/10.1021/acsmedchemlett.9b00493