Design, synthesis, and biological evaluation of F-18-labelled 2, 4-diaminopyrimidine-type FAK-targeted inhibitors as potential tumour imaging agents.
Aminopyridines
/ chemical synthesis
Animals
Drug Design
Female
Fluorine Radioisotopes
/ chemistry
Focal Adhesion Kinase 1
/ antagonists & inhibitors
Humans
Mice
Molecular Docking Simulation
Molecular Structure
Neoplasms
/ diagnostic imaging
Protein Binding
Protein Kinase Inhibitors
/ chemical synthesis
Radiopharmaceuticals
/ chemical synthesis
Structure-Activity Relationship
F-18 labelled
FAK inhibitor
Tumour imaging agents
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
01 10 2020
01 10 2020
Historique:
received:
01
04
2020
revised:
20
07
2020
accepted:
24
07
2020
pubmed:
1
8
2020
medline:
22
6
2021
entrez:
1
8
2020
Statut:
ppublish
Résumé
As a type of intracellular nonreceptor tyrosine kinase, focal adhesion kinase (FAK) can be highly expressed in most types of tumours and is thus regarded as a promising antitumour target. In this study, a series of novel 2,4-diaminopyrimidine FAK-targeted inhibitors were designed, synthesized and characterized by
Identifiants
pubmed: 32736076
pii: S0960-894X(20)30563-1
doi: 10.1016/j.bmcl.2020.127452
pii:
doi:
Substances chimiques
Aminopyridines
0
Fluorine Radioisotopes
0
Protein Kinase Inhibitors
0
Radiopharmaceuticals
0
Focal Adhesion Kinase 1
EC 2.7.10.2
PTK2 protein, human
EC 2.7.10.2
Fluorine-18
GZ5I74KB8G
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
127452Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.