Discovery of 1-Amino-1
Agammaglobulinaemia Tyrosine Kinase
/ antagonists & inhibitors
Antineoplastic Agents
/ pharmacology
Apoptosis
/ drug effects
Cell Line, Tumor
Cytochrome P-450 Enzyme Inhibitors
/ pharmacology
Drug Discovery
Humans
Imidazoles
/ pharmacology
Molecular Docking Simulation
Protein Kinase Inhibitors
/ pharmacology
Signal Transduction
/ drug effects
Structure-Activity Relationship
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 11 2021
11 11 2021
Historique:
pubmed:
22
10
2021
medline:
1
2
2022
entrez:
21
10
2021
Statut:
ppublish
Résumé
Bruton's tyrosine kinase (BTK) inhibitors suppressing the aberrant activation of BTK have led to a paradigm shift in the therapy of B-cell malignancies. However, there is an urgent need to discover more selective covalent BTK inhibitors owing to the off-target adverse effects of the approved inhibitor, ibrutinib. Herein, we disclose the discovery and preliminary activity studies of novel BTK inhibitors carrying 1-amino-1
Identifiants
pubmed: 34672559
doi: 10.1021/acs.jmedchem.1c01559
doi:
Substances chimiques
Antineoplastic Agents
0
Cytochrome P-450 Enzyme Inhibitors
0
Imidazoles
0
Protein Kinase Inhibitors
0
Agammaglobulinaemia Tyrosine Kinase
EC 2.7.10.2
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM