Identification of the 2-Benzoxazol-2-yl-phenol Scaffold as New Hit for JMJD3 Inhibition.
Journal
ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073
Informations de publication
Date de publication:
11 Apr 2019
11 Apr 2019
Historique:
received:
29
11
2018
accepted:
25
02
2019
entrez:
19
4
2019
pubmed:
19
4
2019
medline:
19
4
2019
Statut:
epublish
Résumé
JMJD3 is a member of the KDM6 subfamily and catalyzes the demethylation of lysine 27 on histone H3 (H3K27). This protein was identified as a useful tool in understanding the role of epigenetics in inflammatory conditions and in cancer as well. Guided by a virtual fragment screening approach, we identified the benzoxazole scaffold as a new hit suitable for the development of tighter JMJD3 inhibitors. Compounds were synthesized by a microwave-assisted one-pot reaction under catalyst and solvent-free conditions. Among these, compound
Identifiants
pubmed: 30996803
doi: 10.1021/acsmedchemlett.8b00589
pmc: PMC6466828
doi:
Types de publication
Journal Article
Langues
eng
Pagination
601-605Subventions
Organisme : Versus Arthritis
ID : 20522
Pays : United Kingdom
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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