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Virtual fragment screening identification of a novel Quinoline-5,8-dicarboxylic acid derivative as selective JMJD3 inhibitor.

Abstract:
The quinoline-5,8 dicarboxylic acid scaffold has been identified by fragment-based approach as new potential lead compound for the development of JMJD3 inhibitors. Among them, compound 3 shows low micromolar inhibitory activity against JMJD3. The experimental evaluation of inhibition activity vs. related seven isoforms of JMJD3 highlighted an unprecedented selectivity towards the biological target of interest.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1002/cmdc.201800198

Authors


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Institution:
University of Oxford
Division:
MSD
Department:
NDORMS
Oxford college:
St Catherine's College
Role:
Author
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Name:
Italian Association for Cancer Research
Publisher:
Wiley
Journal:
ChemMedChem More from this journal
Volume:
13
Issue:
12
Pages:
1160-1164
Publication date:
2018-04-06
Acceptance date:
2018-04-03
DOI:
EISSN:
1860-7187
ISSN:
1860-7179
Pmid:
29633584
Language:
English
Keywords:
Pubs id:
pubs:843562
UUID:
uuid:6b7c0653-cada-4dff-9680-39e20b525b12
Local pid:
pubs:843562
Deposit date:
2018-05-02

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