Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.
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:
12 08 2021
12 08 2021
Historique:
pubmed:
15
7
2021
medline:
21
10
2021
entrez:
14
7
2021
Statut:
ppublish
Résumé
Herein, a series of 2,3-dihydrobenzofurans have been developed as highly potent bromo and extra-terminal domain (BET) inhibitors with 1000-fold selectivity for the second bromodomain (BD2) over the first bromodomain (BD1). Investment in the development of two orthogonal synthetic routes delivered inhibitors that were potent and selective but had raised
Identifiants
pubmed: 34260229
doi: 10.1021/acs.jmedchem.1c00344
doi:
Substances chimiques
Benzofurans
0
Proteins
0
bromodomain and extra-terminal domain protein, human
0
coumaran
99E861415L
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM