Synthesis and biological evaluation of selected 7H-pyrrolo[2,3-d]pyrimidine derivatives as novel CDK9/CyclinT and Haspin inhibitors.
Antineoplastic Agents
/ pharmacology
Cell Line, Tumor
Cyclin T
/ antagonists & inhibitors
Cyclin-Dependent Kinase 9
/ antagonists & inhibitors
Humans
Intracellular Signaling Peptides and Proteins
/ antagonists & inhibitors
Molecular Docking Simulation
Protein Serine-Threonine Kinases
/ antagonists & inhibitors
Pyrimidines
/ chemical synthesis
Spectrum Analysis
/ methods
7-Deazapurine
Anticancer
CDK9/CylinT
Haspin
Protein kinase
Journal
Chemico-biological interactions
ISSN: 1872-7786
Titre abrégé: Chem Biol Interact
Pays: Ireland
ID NLM: 0227276
Informations de publication
Date de publication:
01 Nov 2021
01 Nov 2021
Historique:
received:
30
05
2021
revised:
07
08
2021
accepted:
06
09
2021
pubmed:
12
9
2021
medline:
9
11
2021
entrez:
11
9
2021
Statut:
ppublish
Résumé
Protein kinases, including CDK9/CyclinT and Haspin, are regarded as potential drug targets in cancer therapy. Findings from a previous study suggested 7-azaindole as a privileged scaffold for producing inhibitors of CDK9/CyclinT and Haspin. Inspired by these findings, the current study synthesised and evaluated thirteen (13) C6-substituted 7-azaindole and twenty (20) C4-substituted structurally related 7H-pyrrolo[2,3-d]pyrimidine derivatives against a panel of protein kinases, including CDK9/CyclinT and Haspin. Eleven of the 7H-pyrrolo[2,3-d]pyrimidine derivatives exhibited activity toward CDK9/CyclinT, while 4 of compounds had activity against Haspin. The best CDK9/CyclinT (IC
Identifiants
pubmed: 34508710
pii: S0009-2797(21)00281-7
doi: 10.1016/j.cbi.2021.109643
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Cyclin T
0
Intracellular Signaling Peptides and Proteins
0
Pyrimidines
0
HASPIN protein, human
EC 2.7.11.1
Protein Serine-Threonine Kinases
EC 2.7.11.1
CDK9 protein, human
EC 2.7.11.22
Cyclin-Dependent Kinase 9
EC 2.7.11.22
pyrimidine
K8CXK5Q32L
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
109643Informations de copyright
Copyright © 2021 Elsevier B.V. All rights reserved.