Potent Dual Inhibitors of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 with a Suitable Pharmacokinetic Profile for

Female Humans Mice Animals Steryl-Sulfatase Enzyme Inhibitors / pharmacology Endometriosis / drug therapy HEK293 Cells 17-Hydroxysteroid Dehydrogenases Estrogens / metabolism

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:
13 07 2023
Historique:
medline: 14 7 2023
pubmed: 27 6 2023
entrez: 27 6 2023
Statut: ppublish

Résumé

Treating estrogen-dependent diseases like endometriosis with drugs suppressing local estrogen activation may be superior to existing endocrine therapies. Steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) are key enzymes of local estrogen activation. We describe the rational design, synthesis, and biological profilation of furan-based compounds as a novel class of dual STS/17β-HSD1 inhibitors (DSHIs). In T47D cells, compound

Identifiants

DOI: 10.1021/acs.jmedchem.3c00571 PMID: 37369108
pubmed: 37369108
doi: 10.1021/acs.jmedchem.3c00571
doi:

Substances chimiques

3 (or 17)-beta-hydroxysteroid dehydrogenase EC 1.1.1.51
Steryl-Sulfatase EC 3.1.6.2
Enzyme Inhibitors 0
17-Hydroxysteroid Dehydrogenases EC 1.1.-
Estrogens 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

8975-8992

Auteurs

Mohamed Salah (M)

Department of Pharmacy, Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, 66123 Saarbrücken, Germany.
Department of Pharmaceutical Chemistry, School of Pharmacy, Newgiza University (NGU), Newgiza, km 22 Cairo-Alexandria Desert Road, 12577 Cairo, Egypt.
ORCID: 0000-0002-9535-6741

Mariam Tahoun (M)

Department of Pharmacy, Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, 66123 Saarbrücken, Germany.
PharmaCenter Bonn, Pharmaceutical Institute, Department of Pharmaceutical and Medicinal Chemistry, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.
ORCID: 0000-0001-8787-0399

Jeannette Rudzitis-Auth (J)

Institute for Clinical and Experimental Surgery, Saarland University, 66421 Homburg, Germany.

Lisa Stotz (L)

Department of Obstetrics & Gynecology, Saarland University Hospital, 66421 Homburg, Germany.

Chris J van Koppen (CJ)

ElexoPharm GmbH, Campus A12, 66123 Saarbrücken, Germany.
ORCID: 0000-0003-2799-6728

Matthias W Laschke (MW)

Institute for Clinical and Experimental Surgery, Saarland University, 66421 Homburg, Germany.

Ahmed S Abdelsamie (AS)

Department of Chemistry of Natural and Microbial Products, Institute of Pharmaceutical and Drug Industries Research, National Research Centre, El-Buhouth St., Dokki, P.O. Box 12622 Cairo, Egypt.
Department of Drug Design and Optimization, Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) - Helmholtz Centre for Infection Research (HZI), Campus E81, 66123 Saarbrücken, Germany.
ORCID: 0000-0002-5326-4400

Martin Frotscher (M)

Department of Pharmacy, Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, 66123 Saarbrücken, Germany.
ORCID: 0000-0003-1777-8890

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Potent Dual Inhibitors of Steroid Sulfatase...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Potent Dual Inhibitors of Steroid Sulfatase...
questionsmedicales.fr › Eucaryotes › Animaux › Potent Dual Inhibitors of Steroid Sulfatase...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Esterases › Sulfuric ester hydrolases › Arylsulfatases › Steryl-Sulfatase › Potent Dual Inhibitors of Steroid Sulfatase...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Potent Dual Inhibitors of Steroid Sulfatase...
questionsmedicales.fr › Maladies urogénitales › Maladies génitales › Maladies de l'appareil génital féminin › Endométriose › Potent Dual Inhibitors of Steroid Sulfatase...
questionsmedicales.fr › Cellules › Cellules épithéliales › Cellules HEK293 › Potent Dual Inhibitors of Steroid Sulfatase...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Oxidoreductases › Alcohol oxidoreductases › Hydroxysteroid dehydrogenases › 17-Hydroxysteroid dehydrogenases › Potent Dual Inhibitors of Steroid Sulfatase...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Hormones, substituts d'hormones et antagonistes d'hormones › Hormones › Oestrogènes › Potent Dual Inhibitors of Steroid Sulfatase...