Discovery of novel pyruvate dehydrogenase kinases inhibitors by screening of an in-house small molecule library for anti-lung cancer therapeutics.
Antineoplastic Agents
/ chemical synthesis
Cell Line, Tumor
Cell Proliferation
/ drug effects
Dose-Response Relationship, Drug
Drug Discovery
Drug Evaluation, Preclinical
Humans
Lung Neoplasms
/ drug therapy
Molecular Docking Simulation
Molecular Structure
Protein Kinase Inhibitors
/ chemical synthesis
Protein Serine-Threonine Kinases
/ antagonists & inhibitors
Pyruvate Dehydrogenase Acetyl-Transferring Kinase
Small Molecule Libraries
/ chemical synthesis
Structure-Activity Relationship
Anticancer
Biochemical assay
Proliferation
Pyruvate dehydrogenase kinase
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:
15 01 2019
15 01 2019
Historique:
received:
28
10
2018
revised:
14
11
2018
accepted:
16
11
2018
pubmed:
25
11
2018
medline:
5
11
2019
entrez:
25
11
2018
Statut:
ppublish
Résumé
Pyruvate dehydrogenase kinases (PDKs) are widely over-expressed in various human solid cancers, making them attractive therapeutic targets for cancer treatment. Herein, we report the identification of structurally novel PDKs inhibitors by screening of an in-house small molecule library. Biochemical assay indicated that the identified compounds 1-4 inhibited PDK1 activity with EC
Identifiants
pubmed: 30470491
pii: S0960-894X(18)30902-8
doi: 10.1016/j.bmcl.2018.11.035
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
PDK1 protein, human
0
Protein Kinase Inhibitors
0
Pyruvate Dehydrogenase Acetyl-Transferring Kinase
0
Small Molecule Libraries
0
Protein Serine-Threonine Kinases
EC 2.7.11.1
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
291-296Informations de copyright
Copyright © 2018 Elsevier Ltd. All rights reserved.