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Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17ß-HSD1 inhibitor with sub-nanomolar IC

Saarland University

First Structure-Activity Relationship of 17ß-Hydroxysteroid Dehydrogenase Type 14 Nonsteroidal Inhibitors and Crystal Structures in Complex with the Enzyme.

Philipps University Marburg

Towards the evaluation in an animal disease model: Fluorinated 17ß-HSD1 inhibitors showing strong activity towards both the human and the rat enzyme.

Saarland University

Ligand-based pharmacophore modeling and virtual screening for the discovery of novel 17ß-hydroxysteroid dehydrogenase 2 inhibitors.

University Of Innsbruck

Metabolic stability optimization and metabolite identification of 2,5-thiophene amide 17ß-hydroxysteroid dehydrogenase type 2 inhibitors.

Saarland University

Inhibition of 17ß-HSD1: SAR of bicyclic substituted hydroxyphenylmethanones and discovery of new potent inhibitors with thioether linker.

Saarland University

Novel, potent and selective 17ß-hydroxysteroid dehydrogenase type 2 inhibitors as potential therapeutics for osteoporosis with dual human and mouse activities.

Saarland University

Novel N-methylsulfonamide and retro-N-methylsulfonamide derivatives as 17ß-hydroxysteroid dehydrogenase type 2 (17ß-HSD2) inhibitors with good ADME-related physicochemical parameters.

Saarland University

Structural optimization of 2,5-thiophene amides as highly potent and selective 17ß-hydroxysteroid dehydrogenase type 2 inhibitors for the treatment of osteoporosis.

Saarland University

Optimization of hydroxybenzothiazoles as novel potent and selective inhibitors of 17ß-HSD1.

Saarland University

Lead optimization of 17ß-HSD1 inhibitors of the (hydroxyphenyl)naphthol sulfonamide type for the treatment of endometriosis.

Saarland University

Discovery of nonsteroidal 17beta-hydroxysteroid dehydrogenase 1 inhibitors by pharmacophore-based screening of virtual compound libraries.

University Of Innsbruck

Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases.

Saarland University

4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17beta-hydroxysteroid dehydrogenase. Part 3. Identification of lead candidate.

Bayer Research Center

 

3-Hydroxy-19-nor-17-pregna-1,3,5(10)-triene-21,17-carbolactone as inhibitor of 17-hydroxysteroid dehydrogenase type 2

TBA

Discovery of a new class of bicyclic substituted hydroxyphenylmethanones as 17ß-hydroxysteroid dehydrogenase type 2 (17ß-HSD2) inhibitors for the treatment of osteoporosis.

Saarland University

Triazole ring-opening leads to the discovery of potent nonsteroidal 17ß-hydroxysteroid dehydrogenase type 2 inhibitors.

Saarland University

Introduction of an electron withdrawing group on the hydroxyphenylnaphthol scaffold improves the potency of 17ß-hydroxysteroid dehydrogenase type 2 (17ß-HSD2) inhibitors.

Saarland University

New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17ß-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases.

Saarland University

17ß-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold.

Saarland University

Bicyclic substituted hydroxyphenylmethanones as novel inhibitors of 17ß-hydroxysteroid dehydrogenase type 1 (17ß-HSD1) for the treatment of estrogen-dependent diseases.

Saarland University

Discovery and optimization of adamantyl carbamate inhibitors of 11ß-HSD1.

Vitae Pharmaceuticals

Novel estrone mimetics with high 17beta-HSD1 inhibitory activity.

Saarland University And Helmholtz Institute For Pharmaceutical Research Saarland (Hips)

New insights into the SAR and binding modes of bis(hydroxyphenyl)thiophenes and -benzenes: influence of additional substituents on 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitory activity and selectivity.

Saarland University

Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes.

Amgen

Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics.

Saarland University

Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases.

Saarland University

The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening.

University Of Innsbruck

4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17beta-hydroxysteroid dehydrogenase. Part 2. SAR.

Bayer Research Center

Targeted Endocrine Therapy: Design, Synthesis, and Proof-of-Principle of 17?-Hydroxysteroid Dehydrogenase Type 2 Inhibitors in Bone Fracture Healing.

Elexopharm

Development of potential preclinical candidates with promising in vitro ADME profile for the inhibition of type 1 and type 2 17?-Hydroxysteroid dehydrogenases: Design, synthesis, and biological evaluation.

Helmholtz Institute For Pharmaceutical Research Saarland (Hips)

Design, Synthesis, and Biological Characterization of Orally Active 17?-Hydroxysteroid Dehydrogenase Type 2 Inhibitors Targeting the Prevention of Osteoporosis.

Elexopharm

Addressing cytotoxicity of 1,4-biphenyl amide derivatives: Discovery of new potent and selective 17?-hydroxysteroid dehydrogenase type 2 inhibitors.

Saarland University

Highly Potent 17?-HSD2 Inhibitors with a Promising Pharmacokinetic Profile for Targeted Osteoporosis Therapy.

Pharmbiotec

Potential Antiosteoporotic Natural Product Lead Compounds That Inhibit 17?-Hydroxysteroid Dehydrogenase Type 2.

University Of Basel

First Dual Inhibitors of Steroid Sulfatase (STS) and 17?-Hydroxysteroid Dehydrogenase Type 1 (17?-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.

Saarland University

Phenylbenzenesulfonates and -sulfonamides as 17?-hydroxysteroid dehydrogenase type 2 inhibitors: Synthesis and SAR-analysis.

University Of Innsbruck

A comparison between dopamine-stimulated adenylate cyclase and 3H-SCH 23390 binding in rat striatum.

UniversitÉ