Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor.
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
09 07 2020
09 07 2020
Historique:
pubmed:
9
6
2020
medline:
18
11
2020
entrez:
9
6
2020
Statut:
ppublish
Résumé
Tankyrases 1 and 2 are central biotargets in the WNT/β-catenin signaling and Hippo signaling pathways. We have previously developed tankyrase inhibitors bearing a 1,2,4-triazole moiety and binding predominantly to the adenosine binding site of the tankyrase catalytic domain. Here we describe a systematic structure-guided lead optimization approach of these tankyrase inhibitors. The central 1,2,4-triazole template and
Identifiants
pubmed: 32511917
doi: 10.1021/acs.jmedchem.0c00208
pmc: PMC8008393
doi:
Substances chimiques
Poly(ADP-ribose) Polymerase Inhibitors
0
Triazoles
0
Tankyrases
EC 2.4.2.30
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
6834-6846Références
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