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Identification of the 2-benzoxazol-2-yl-phenol scaffold as new hit for JMJD3 inhibition

Abstract:

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...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher:
American Chemical Society
Journal:
ACS Medicinal Chemistry Letters More from this journal
Volume:
10
Issue:
4
Pages:
601-605
Publication date:
2019-02-25
Acceptance date:
2019-02-25
DOI:
EISSN:
1948-5875
ISSN:
1948-5875
Pmid:
30996803
Language:
English
Keywords:
Pubs id:
pubs:993234
UUID:
uuid:c986cf06-c021-4aa2-a4bc-87f631bd7f16
Local pid:
pubs:993234
Source identifiers:
993234
Deposit date:
2019-04-25

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