Discovery of Thieno[2,3-
Animals
Antineoplastic Agents
/ chemical synthesis
Apoptosis
/ drug effects
Autophagy
/ drug effects
Cell Cycle Proteins
/ antagonists & inhibitors
Cell Line, Tumor
Cell Proliferation
/ drug effects
Colorectal Neoplasms
/ drug therapy
Drug Design
Drug Screening Assays, Antitumor
Female
Histone Deacetylase Inhibitors
/ chemical synthesis
Histone Deacetylases
/ metabolism
Humans
Hydroxamic Acids
/ chemical synthesis
Male
Molecular Docking Simulation
Molecular Structure
Pyrimidines
/ chemical synthesis
Rats, Sprague-Dawley
Signal Transduction
/ drug effects
Structure-Activity Relationship
Thiophenes
/ chemical synthesis
Transcription Factors
/ antagonists & inhibitors
Xenograft Model Antitumor Assays
Zebrafish
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:
09 04 2020
09 04 2020
Historique:
pubmed:
11
3
2020
medline:
8
10
2020
entrez:
11
3
2020
Statut:
ppublish
Résumé
Bromodomain-containing protein 4 (BRD4) and histone deacetylases (HDAC) are both attractive epigenetic targets in cancer and other chronic diseases. Based on the integrated fragment-based drug design, synthesis, and in vitro and in vivo evaluations, a series of novel thieno[2,3-
Identifiants
pubmed: 32153186
doi: 10.1021/acs.jmedchem.9b02178
doi:
Substances chimiques
Antineoplastic Agents
0
BRD4 protein, human
0
Cell Cycle Proteins
0
Histone Deacetylase Inhibitors
0
Hydroxamic Acids
0
Pyrimidines
0
Thiophenes
0
Transcription Factors
0
Histone Deacetylases
EC 3.5.1.98
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM