PMID

Data

Article Title

Organization

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

Identification of fused 16ß,17ß-oxazinone-estradiol derivatives as a new family of non-estrogenic 17ß-hydroxysteroid dehydrogenase type 1 inhibitors.

Universit£

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

Hydroxybenzothiophene Ketones Are Efficient Pre-mRNA Splicing Modulators Due to Dual Inhibition of Dyrk1A and Clk1/4.

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

Synopsis of some recent tactical application of bioisosteres in drug design.

Bristol-Myers Squibb Pharmaceutical Research and Development

Crucial Role of 3-Bromoethyl in Removing the Estrogenic Activity of 17ß-HSD1 Inhibitor 16ß-(m-Carbamoylbenzyl)estradiol.

TBA

Free-Wilson and structural approaches to co-optimizing human and rodent isoform potency for 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors.

Astrazeneca

Novel acidic 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitor with reduced acyl glucuronide liability: the discovery of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid (AZD8329).

Astrazeneca

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

Saarland University

Discovery of a potent, selective, and orally bioavailable acidic 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017).

Astrazeneca

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

Saarland University

Structure-based design, synthesis and in vitro characterization of potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors based on 2-substitutions of estrone and D-homo-estrone.

Institute of Experimental Genetics

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

University of Innsbruck

Novel inhibitors of 17beta-hydroxysteroid dehydrogenase type 1: templates for design.

University of Bath

Estradiol and estrone C-16 derivatives as inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: blocking of ER+ breast cancer cell proliferation induced by estrone.

Chuq-Pavillon Chul and Universit£

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

Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.

University of Bath

E-ring modified steroids as novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.

University of Bath

Novel and potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors.

University of Bath

 

16-propyl derivatives of estradiol as inhibitors of 17-hydroxysteroid dehydrogenase type 1

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

Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1.

Vitae Pharmaceuticals

Synthesis and preliminary evaluation of a modified estradiol-core bearing a fused¿-lactone as non-estrogenic inhibitor of 17ß-hydroxysteroid dehydrogenase type 1.

Chuq - Research Center and Laval 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

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

Design and synthesis of bisubstrate inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: overview and perspectives.

Chuq-Pavillon Chul and Université

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

University of Innsbruck

Estradiol-adenosine hybrid compounds designed to inhibit type 1 17beta-hydroxysteroid dehydrogenase.

Chuq-Pavillon Chul and Université

Dual Targeting of Steroid Sulfatase and 17?-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis.

Saarland University

17?-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer.

Saarland University

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

Discovery of a non-estrogenic irreversible inhibitor of 17?-hydroxysteroid dehydrogenase type 1 from 3-substituted-16?-(m-carbamoylbenzyl)-estradiol derivatives.

Laval 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

Trifluoromethylacetylenic alcohols as affinity labels: inactivation of estradiol dehydrogenase by a trifluoromethylacetylenic secostradiol.

Washington University

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

Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11? hydroxysteroid dehydrogenase type 1 inhibitor.

Vitae Pharmaceuticals

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

UniversitÉ