Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with
Animals
Antineoplastic Agents
/ chemistry
Cell Line, Tumor
Cell Proliferation
/ drug effects
DNA (Cytosine-5-)-Methyltransferase 1
/ antagonists & inhibitors
Drug Design
Enzyme Inhibitors
/ chemistry
Histocompatibility Antigens
/ metabolism
Histone Deacetylase Inhibitors
/ chemistry
Histone Deacetylases
/ metabolism
Histone-Lysine N-Methyltransferase
/ antagonists & inhibitors
Humans
Mice, Inbred BALB C
Molecular Docking Simulation
Neoplasms
/ drug therapy
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:
25 03 2021
25 03 2021
Historique:
pubmed:
5
3
2021
medline:
5
6
2021
entrez:
4
3
2021
Statut:
ppublish
Résumé
Concomitant inhibition of key epigenetic pathways involved in silencing tumor suppressor genes has been recognized as a promising strategy for cancer therapy. Herein, we report a first-in-class series of quinoline-based analogues that simultaneously inhibit histone deacetylases (from a low nanomolar range) and DNA methyltransferase-1 (from a mid-nanomolar range, IC
Identifiants
pubmed: 33661013
doi: 10.1021/acs.jmedchem.0c02255
doi:
Substances chimiques
Antineoplastic Agents
0
Enzyme Inhibitors
0
Histocompatibility Antigens
0
Histone Deacetylase Inhibitors
0
DNA (Cytosine-5-)-Methyltransferase 1
EC 2.1.1.37
DNMT1 protein, human
EC 2.1.1.37
EHMT2 protein, human
EC 2.1.1.43
Histone-Lysine N-Methyltransferase
EC 2.1.1.43
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