The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 27852458 |
64 |
Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17ß-HSD1 inhibitor with sub-nanomolar IC |
Saarland University |
| 27933965 |
39 |
First Structure-Activity Relationship of 17ß-Hydroxysteroid Dehydrogenase Type 14 Nonsteroidal Inhibitors and Crystal Structures in Complex with the Enzyme. |
Philipps University Marburg |
| 26322835 |
96 |
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 |
| 25728028 |
2 |
Identification of fused 16ß,17ß-oxazinone-estradiol derivatives as a new family of non-estrogenic 17ß-hydroxysteroid dehydrogenase type 1 inhibitors. |
Universit£ |
| 24960438 |
24 |
Ligand-based pharmacophore modeling and virtual screening for the discovery of novel 17ß-hydroxysteroid dehydrogenase 2 inhibitors. |
University of Innsbruck |
| 25259513 |
34 |
Metabolic stability optimization and metabolite identification of 2,5-thiophene amide 17ß-hydroxysteroid dehydrogenase type 2 inhibitors. |
Saarland University |
| 25221649 |
47 |
Hydroxybenzothiophene Ketones Are Efficient Pre-mRNA Splicing Modulators Due to Dual Inhibition of Dyrk1A and Clk1/4. |
Saarland University |
| 24929290 |
19 |
Inhibition of 17ß-HSD1: SAR of bicyclic substituted hydroxyphenylmethanones and discovery of new potent inhibitors with thioether linker. |
Saarland University |
| 24974351 |
36 |
Novel, potent and selective 17ß-hydroxysteroid dehydrogenase type 2 inhibitors as potential therapeutics for osteoporosis with dual human and mouse activities. |
Saarland University |
| 24036043 |
22 |
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 |
| 23145773 |
45 |
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 |
| 21413808 |
170 |
Synopsis of some recent tactical application of bioisosteres in drug design. |
Bristol-Myers Squibb Pharmaceutical Research and Development |
| 21927646 |
3 |
Crucial Role of 3-Bromoethyl in Removing the Estrogenic Activity of 17ß-HSD1 Inhibitor 16ß-(m-Carbamoylbenzyl)estradiol. |
TBA |
| 23153367 |
92 |
Free-Wilson and structural approaches to co-optimizing human and rodent isoform potency for 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors. |
Astrazeneca |
| 23088558 |
36 |
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 |
| 22277094 |
59 |
Optimization of hydroxybenzothiazoles as novel potent and selective inhibitors of 17ß-HSD1. |
Saarland University |
| 22691057 |
32 |
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 |
| 22380653 |
69 |
Lead optimization of 17ß-HSD1 inhibitors of the (hydroxyphenyl)naphthol sulfonamide type for the treatment of endometriosis. |
Saarland University |
| 19836949 |
31 |
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 |
| 18533708 |
25 |
Discovery of nonsteroidal 17beta-hydroxysteroid dehydrogenase 1 inhibitors by pharmacophore-based screening of virtual compound libraries. |
University of Innsbruck |
| 18329273 |
14 |
Novel inhibitors of 17beta-hydroxysteroid dehydrogenase type 1: templates for design. |
University of Bath |
| 18035543 |
4 |
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£ |
| 18324762 |
20 |
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 |
| 16480268 |
15 |
Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. |
University of Bath |
| 16134943 |
15 |
E-ring modified steroids as novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. |
University of Bath |
| 15828812 |
3 |
Novel and potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors. |
University of Bath |
| | 5 |
16-propyl derivatives of estradiol as inhibitors of 17-hydroxysteroid dehydrogenase type 1 |
TBA |
| 21945251 |
32 |
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 |
| 22037253 |
51 |
Triazole ring-opening leads to the discovery of potent nonsteroidal 17ß-hydroxysteroid dehydrogenase type 2 inhibitors. |
Saarland University |
| 21972996 |
21 |
Introduction of an electron withdrawing group on the hydroxyphenylnaphthol scaffold improves the potency of 17ß-hydroxysteroid dehydrogenase type 2 (17ß-HSD2) inhibitors. |
Saarland University |
| 21786805 |
130 |
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1. |
Vitae Pharmaceuticals |
| 21782424 |
1 |
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 |
| 21189020 |
54 |
New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17ß-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases. |
Saarland University |
| 21211981 |
8 |
17ß-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold. |
Saarland University |
| 20977238 |
46 |
Bicyclic substituted hydroxyphenylmethanones as novel inhibitors of 17ß-hydroxysteroid dehydrogenase type 1 (17ß-HSD1) for the treatment of estrogen-dependent diseases. |
Saarland University |
| 20413314 |
14 |
Novel estrone mimetics with high 17beta-HSD1 inhibitory activity. |
Saarland University and Helmholtz Institute For Pharmaceutical Research Saarland (Hips) |
| 19831396 |
84 |
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 |
| 18652443 |
11 |
Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. |
Amgen |
| 18630892 |
6 |
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 |
| 18514529 |
11 |
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 |
| 18372081 |
11 |
Design and synthesis of bisubstrate inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: overview and perspectives. |
Chuq-Pavillon Chul and Université |
| 16759088 |
38 |
The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening. |
University of Innsbruck |
| 16366595 |
10 |
Estradiol-adenosine hybrid compounds designed to inhibit type 1 17beta-hydroxysteroid dehydrogenase. |
Chuq-Pavillon Chul and Université |
| 30645111 |
48 |
Targeted Endocrine Therapy: Design, Synthesis, and Proof-of-Principle of 17?-Hydroxysteroid Dehydrogenase Type 2 Inhibitors in Bone Fracture Healing. |
Elexopharm |
| 31176098 |
33 |
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) |
| 31343176 |
72 |
Design, Synthesis, and Biological Characterization of Orally Active 17?-Hydroxysteroid Dehydrogenase Type 2 Inhibitors Targeting the Prevention of Osteoporosis. |
Elexopharm |
| 26615885 |
10 |
Addressing cytotoxicity of 1,4-biphenyl amide derivatives: Discovery of new potent and selective 17?-hydroxysteroid dehydrogenase type 2 inhibitors. |
Saarland University |
| 24328103 |
9 |
Discovery of a non-estrogenic irreversible inhibitor of 17?-hydroxysteroid dehydrogenase type 1 from 3-substituted-16?-(m-carbamoylbenzyl)-estradiol derivatives. |
Laval University |
| 30480443 |
77 |
Highly Potent 17?-HSD2 Inhibitors with a Promising Pharmacokinetic Profile for Targeted Osteoporosis Therapy. |
Pharmbiotec |
| 28319389 |
31 |
Potential Antiosteoporotic Natural Product Lead Compounds That Inhibit 17?-Hydroxysteroid Dehydrogenase Type 2. |
University of Basel |
| 2391679 |
3 |
Trifluoromethylacetylenic alcohols as affinity labels: inactivation of estradiol dehydrogenase by a trifluoromethylacetylenic secostradiol. |
Washington University |
| 28406629 |
51 |
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 |
| 28528082 |
140 |
Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11? hydroxysteroid dehydrogenase type 1 inhibitor. |
Vitae Pharmaceuticals |
| 2415793 |
55 |
A comparison between dopamine-stimulated adenylate cyclase and 3H-SCH 23390 binding in rat striatum. |
UniversitÉ |
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