Optimization of Covalent MKK7 Inhibitors
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:
11 08 2022
11 08 2022
Historique:
pubmed:
2
8
2022
medline:
13
8
2022
entrez:
1
8
2022
Statut:
ppublish
Résumé
High-throughput nanomole-scale synthesis allows for late-stage functionalization (LSF) of compounds in an efficient and economical manner. Here, we demonstrated that copper-catalyzed azide-alkyne cycloaddition could be used for the LSF of covalent kinase inhibitors at the nanoscale, enabling the synthesis of hundreds of compounds that did not require purification for biological assay screening, thus reducing experimental time drastically. We generated crude libraries of inhibitors for the kinase MKK7, derived from two different parental precursors, and analyzed them
Identifiants
pubmed: 35912476
doi: 10.1021/acs.jmedchem.1c02206
pmc: PMC9376956
doi:
Substances chimiques
Alkynes
0
Azides
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
10341-10356Références
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