Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis.
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:
08 09 2022
08 09 2022
Historique:
pubmed:
23
8
2022
medline:
11
9
2022
entrez:
22
8
2022
Statut:
ppublish
Résumé
A novel approach for the dual inhibition of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1(17β HSD1) by a single drug was explored, starting from in-house 17β HSD1 inhibitors via masking their phenolic OH group with a sulfamate ester. The sulfamates were intentionally designed as drugs for the inhibition of STS and, at the same time, prodrugs for 17β-HSD1 inhibition ("drug-prodrug approach"). The most promising sulfamates
Identifiants
pubmed: 35993890
doi: 10.1021/acs.jmedchem.2c00589
doi:
Substances chimiques
Enzyme Inhibitors
0
Phenols
0
Prodrugs
0
17-Hydroxysteroid Dehydrogenases
EC 1.1.-
3 (or 17)-beta-hydroxysteroid dehydrogenase
EC 1.1.1.51
Steryl-Sulfatase
EC 3.1.6.2
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM