Optimization of 4,6-Disubstituted Pyrido[3,2-
Animals
Antineoplastic Agents
/ chemistry
Apoptosis
/ drug effects
Cell Line, Tumor
Cell Proliferation
/ drug effects
G1 Phase Cell Cycle Checkpoints
/ drug effects
Humans
Intracellular Signaling Peptides and Proteins
/ antagonists & inhibitors
Leukemia, Myeloid
/ drug therapy
Male
Mice, Inbred NOD
Mice, SCID
Molecular Docking Simulation
Protein Binding
Protein Kinase Inhibitors
/ chemistry
Protein Serine-Threonine Kinases
/ antagonists & inhibitors
Proto-Oncogene Proteins c-pim-1
/ antagonists & inhibitors
Pyridines
/ chemistry
Pyrimidines
/ chemistry
Rats, Sprague-Dawley
Xenograft Model Antitumor Assays
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:
23 09 2021
23 09 2021
Historique:
pubmed:
14
9
2021
medline:
15
12
2021
entrez:
13
9
2021
Statut:
ppublish
Résumé
Mitogen-activated protein kinase-interacting kinases (MNKs) and provirus integration in maloney murine leukemia virus kinases (PIMs) are downstream enzymes of cell proliferation signaling pathways associated with the resistance of tyrosine kinase inhibitors. MNKs and PIMs have complementary effects to regulate cap-dependent translation of oncoproteins. Dual inhibitors of MNKs and PIMs have not been developed. We developed a novel 4,6-disubstituted pyrido[3,2-
Identifiants
pubmed: 34515481
doi: 10.1021/acs.jmedchem.1c01084
doi:
Substances chimiques
Antineoplastic Agents
0
Intracellular Signaling Peptides and Proteins
0
Protein Kinase Inhibitors
0
Pyridines
0
Pyrimidines
0
MKNK1 protein, human
EC 2.7.1.-
MKNK2 protein, human
EC 2.7.11.1
PIM1 protein, human
EC 2.7.11.1
Protein Serine-Threonine Kinases
EC 2.7.11.1
Proto-Oncogene Proteins c-pim-1
EC 2.7.11.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM