Novel androgen receptor antagonist identified by structure-based virtual screening, structural optimization, and biological evaluation.
3T3 Cells
Androgen Receptor Antagonists
/ chemical synthesis
Animals
Cell Proliferation
/ drug effects
Cell Survival
/ drug effects
Dose-Response Relationship, Drug
Drug Evaluation, Preclinical
Drug Screening Assays, Antitumor
Humans
Mice
Molecular Docking Simulation
Molecular Structure
Quinolones
/ chemical synthesis
Structure-Activity Relationship
Tumor Cells, Cultured
Androgen receptor
Antagonist
Molecular docking
Prostate cancer
Structure-based virtual screening
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
15 Apr 2020
15 Apr 2020
Historique:
received:
23
12
2019
revised:
07
02
2020
accepted:
16
02
2020
pubmed:
3
3
2020
medline:
1
12
2020
entrez:
2
3
2020
Statut:
ppublish
Résumé
Androgen receptor (AR) plays important roles in the development of prostate cancer (PCa), and therefore it has been regarded as the most important therapeutic target for both hormone-sensitive prostate cancer (HSPC) and advanced PCa. In this study, a novel hit (C18) with IC
Identifiants
pubmed: 32114360
pii: S0223-5234(20)30123-9
doi: 10.1016/j.ejmech.2020.112156
pii:
doi:
Substances chimiques
Androgen Receptor Antagonists
0
Quinolones
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
112156Informations de copyright
Copyright © 2020 Elsevier Masson SAS. 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.