Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T44011 | ||||
Target Name | Estradiol 17 beta-dehydrogenase 1 | ||||
Target Type | Clinical Trial |
||||
Drug Potency against Target | 16-beta-ethoxymethyl-estrone | Drug Info | IC50 = 320 nM | [528033] | |
NARINGENIN | Drug Info | IC50 = 4960 nM | [529519] | ||
6-(4-Hydroxy-phenyl)-naphthalen-1-ol | Drug Info | IC50 = 2425 nM | [529359] | ||
3-(2-naphthyl)phenol | Drug Info | IC50 = 2257 nM | [529359] | ||
3,3'-(1,2,4,5-tetrazine-3,6-diyl)diphenol | Drug Info | IC50 = 201 nM | [529748] | ||
3,3'-(3-Phenylthiene-2,5-diyl)diphenol | Drug Info | IC50 = 493 nM | [530450] | ||
4-[5-(3-Hydroxyphenyl)-3-thienyl]-2-methylphenol | Drug Info | IC50 = 64 nM | [530450] | ||
3,4'-(thiophene-2,4-diyl)diphenol | Drug Info | IC50 = 77 nM | [530450] | ||
NSC-94258 | Drug Info | IC50 = 5250 nM | [529519] | ||
6-(3-Hydroxy-phenyl)-naphthalen-2-ol | Drug Info | IC50 = 116 nM | [529595] | ||
APIGENIN | Drug Info | IC50 = 710 nM | [529519] | ||
1-Bromo-6-(3-hydroxyphenyl)-2-naphthol | Drug Info | IC50 = 40 nM | [529595] | ||
6-(3-Hydroxyphenyl)-1-phenyl-2-naphthol | Drug Info | IC50 = 20 nM | [529595] | ||
BVT.2733 | Drug Info | IC50 = 52 nM | [529615] | ||
KAEMPFEROL | Drug Info | IC50 = 1050 nM | [529519] | ||
3,3'-(1,2,4-Thiadiazol-2,5-diyl)diphenol | Drug Info | IC50 = 336 nM | [529748] | ||
N-(1'-Phenyl-ethyl) estradiol-16-carboxamide | Drug Info | IC50 = 810 nM | [528033] | ||
3-[5-(3,4-Difluorophenyl)-2-thienyl]phenol | Drug Info | IC50 = 780 nM | [530450] | ||
5-(6-hydroxy-2-naphthyl)pyridin-3-ol | Drug Info | IC50 = 1232 nM | [529359] | ||
3,3-(1,3-Thiazole-2,5-diyl)diphenol | Drug Info | IC50 = 243 nM | [529748] | ||
3-Fluoro-5-[5-(4-hydroxyphenyl)-2-thienyl]phenol | Drug Info | IC50 = 42 nM | [530450] | ||
3-[5-(4-hydroxyphenyl)-2-thienyl]phenol | Drug Info | IC50 = 69 nM | [530450] | ||
4-[5-(3-Hydroxyphenyl)-2-thienyl)-2-methyl]phenol | Drug Info | IC50 = 46 nM | [530450] | ||
3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]phenol | Drug Info | IC50 = 310 nM | [529748] | ||
3-[4-(5-Chloro-2-thienyl)pyridin-2-yl]phenol | Drug Info | IC50 = 850 nM | [530868] | ||
N-methyl estrone-16-methyl carboxamide | Drug Info | IC50 = 1500 nM | [528033] | ||
2-Fluoro-5-[5-(4-hydroxyphenyl)-2-thienyl]phenol | Drug Info | IC50 = 113 nM | [530450] | ||
1,1':4',1''-terphenyl-3,3''-diol | Drug Info | IC50 = 173 nM | [530450] | ||
1,1':4',1''-terphenyl-3,4''-diol | Drug Info | IC50 = 471 nM | [530450] | ||
3,3'-pyrazine-2,5-diyldiphenol | Drug Info | IC50 = 1000 nM | [529748] | ||
2-Fluoro-4-[5-(3-hydroxyphenyl)-3-thienyl]phenol | Drug Info | IC50 = 64 nM | [530450] | ||
3-[2-(5-Chloro-2-thienyl)pyridin-4-yl]phenol | Drug Info | IC50 = 2380 nM | [530868] | ||
3,3'-Pyridine-2,5-diyldiphenol | Drug Info | IC50 = 101 nM | [529748] | ||
3-[5-(4-Hydroxyphenyl)-2-thienyl]-5-methylphenol | Drug Info | IC50 = 629 nM | [530450] | ||
4-Fluoro-1,1':4',1''-terphenyl-3,3''-diol | Drug Info | IC50 = 51 nM | [530450] | ||
6-oxo-estrone | Drug Info | IC50 = 340 nM | [528033] | ||
4'-(5-Chloro-2-thienyl)biphenyl-3-ol | Drug Info | IC50 = 1020 nM | [530868] | ||
3'-(5-Chloro-2-thienyl)biphenyl-3-ol | Drug Info | IC50 = 560 nM | [530868] | ||
3-[5-(3-Fluorophenyl)-2-thienyl]phenol | Drug Info | IC50 = 535 nM | [530450] | ||
Ethyl estrone-16-methylcarboxylate | Drug Info | IC50 = 300 nM | [528033] | ||
3,3',3''-Thiene-2,3,5-triyltriphenol | Drug Info | IC50 = 119 nM | [530450] | ||
3-[5-(4-Fluorophenyl)-2-thienyl]phenol | Drug Info | IC50 = 717 nM | [530450] | ||
2-Fluoro-4-[5-(3-hydroxyphenyl)-2-thienyl]phenol | Drug Info | IC50 = 8 nM | [530450] | ||
4-Methyl-1,1':4',1''-terphenyl-3,4''-diol | Drug Info | IC50 = 171 nM | [530450] | ||
3,3'-thiene-2,5-diyldiphenol | Drug Info | IC50 = 173 nM | [530450] | ||
3-[4-(4-Hydroxyphenyl)-1,3-oxazol-2-yl]phenol | Drug Info | IC50 = 1850 nM | [529504] | ||
3-[3-(4-hydroxyphenyl)isoxazol-5-yl]phenol | Drug Info | IC50 = 1610 nM | [529504] | ||
3,3'-(1,3-Thiazol-2,4-diyl)diphenol | Drug Info | IC50 = 455 nM | [529748] | ||
3,3'-(1,2,4-thiadiazole-3,5-diyl)diphenol | Drug Info | IC50 = 169 nM | [529748] | ||
3-[5-(4-Hydroxyphenyl)-3-thienyl]phenol | Drug Info | IC50 = 151 nM | [529748] | ||
3-(5-phenyl-2-thienyl)phenol | Drug Info | IC50 = 342 nM | [530450] | ||
3-[5-(4-hydroxyphenyl)-1,3-thiazol-2-yl]phenol | Drug Info | IC50 = 50 nM | [530450] | ||
4-[5-(3-Hydroxyphenyl)-2-thienyl]benzene-1,2-diol | Drug Info | IC50 = 402 nM | [530450] | ||
4'-(6-Methoxypyridin-3-yl)biphenyl-3-ol | Drug Info | IC50 = 690 nM | [530868] | ||
3-[6-(5-Chloro-2-thienyl)pyridin-2-yl]phenol | Drug Info | IC50 = 1390 nM | [530868] | ||
3'-(1-Benzothien-2-yl)biphenyl-3-ol | Drug Info | IC50 = 1370 nM | [530868] | ||
3,3'-(3-Methylthiene-2,5-diyl]diphenol | Drug Info | IC50 = 567 nM | [530450] | ||
N-(pyridin-3-ylmethyl) estradiol-16-carboxamide | Drug Info | IC50 = 510 nM | [528033] | ||
16-(pyridin-4-yl)methylene-estradiol | Drug Info | IC50 = 4100 nM | [528033] | ||
3,3'-Thiene-2,4-diyldiphenol | Drug Info | IC50 = 185 nM | [529748] | ||
References | |||||
Ref 528033 | J Med Chem. 2006 Feb 23;49(4):1325-45.Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. | ||||
Ref 529519 | J Med Chem. 2008 Jul 24;51(14):4188-99. Epub 2008 Jun 6.Discovery of nonsteroidal 17beta-hydroxysteroid dehydrogenase 1 inhibitors by pharmacophore-based screening of virtual compound libraries. | ||||
Ref 529359 | J Med Chem. 2008 Apr 10;51(7):2158-69. Epub 2008 Mar 7.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. | ||||
Ref 529359 | J Med Chem. 2008 Apr 10;51(7):2158-69. Epub 2008 Mar 7.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. | ||||
Ref 529748 | J Med Chem. 2008 Nov 13;51(21):6725-39. Epub 2008 Oct 15.Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 529519 | J Med Chem. 2008 Jul 24;51(14):4188-99. Epub 2008 Jun 6.Discovery of nonsteroidal 17beta-hydroxysteroid dehydrogenase 1 inhibitors by pharmacophore-based screening of virtual compound libraries. | ||||
Ref 529595 | J Med Chem. 2008 Aug 14;51(15):4685-98. Epub 2008 Jul 17.Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. | ||||
Ref 529519 | J Med Chem. 2008 Jul 24;51(14):4188-99. Epub 2008 Jun 6.Discovery of nonsteroidal 17beta-hydroxysteroid dehydrogenase 1 inhibitors by pharmacophore-based screening of virtual compound libraries. | ||||
Ref 529595 | J Med Chem. 2008 Aug 14;51(15):4685-98. Epub 2008 Jul 17.Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. | ||||
Ref 529595 | J Med Chem. 2008 Aug 14;51(15):4685-98. Epub 2008 Jul 17.Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. | ||||
Ref 529615 | J Med Chem. 2008 Aug 28;51(16):4851-7. Epub 2008 Jul 22.Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. | ||||
Ref 529519 | J Med Chem. 2008 Jul 24;51(14):4188-99. Epub 2008 Jun 6.Discovery of nonsteroidal 17beta-hydroxysteroid dehydrogenase 1 inhibitors by pharmacophore-based screening of virtual compound libraries. | ||||
Ref 529748 | J Med Chem. 2008 Nov 13;51(21):6725-39. Epub 2008 Oct 15.Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). | ||||
Ref 528033 | J Med Chem. 2006 Feb 23;49(4):1325-45.Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 529359 | J Med Chem. 2008 Apr 10;51(7):2158-69. Epub 2008 Mar 7.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. | ||||
Ref 529748 | J Med Chem. 2008 Nov 13;51(21):6725-39. Epub 2008 Oct 15.Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 529748 | J Med Chem. 2008 Nov 13;51(21):6725-39. Epub 2008 Oct 15.Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). | ||||
Ref 530868 | Bioorg Med Chem. 2010 May 15;18(10):3494-505. Epub 2010 Mar 29.Novel estrone mimetics with high 17beta-HSD1 inhibitory activity. | ||||
Ref 528033 | J Med Chem. 2006 Feb 23;49(4):1325-45.Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 529748 | J Med Chem. 2008 Nov 13;51(21):6725-39. Epub 2008 Oct 15.Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530868 | Bioorg Med Chem. 2010 May 15;18(10):3494-505. Epub 2010 Mar 29.Novel estrone mimetics with high 17beta-HSD1 inhibitory activity. | ||||
Ref 529748 | J Med Chem. 2008 Nov 13;51(21):6725-39. Epub 2008 Oct 15.Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 528033 | J Med Chem. 2006 Feb 23;49(4):1325-45.Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. | ||||
Ref 530868 | Bioorg Med Chem. 2010 May 15;18(10):3494-505. Epub 2010 Mar 29.Novel estrone mimetics with high 17beta-HSD1 inhibitory activity. | ||||
Ref 530868 | Bioorg Med Chem. 2010 May 15;18(10):3494-505. Epub 2010 Mar 29.Novel estrone mimetics with high 17beta-HSD1 inhibitory activity. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 528033 | J Med Chem. 2006 Feb 23;49(4):1325-45.Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 529504 | Bioorg Med Chem. 2008 Jun 15;16(12):6423-35. Epub 2008 May 3.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. | ||||
Ref 529504 | Bioorg Med Chem. 2008 Jun 15;16(12):6423-35. Epub 2008 May 3.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. | ||||
Ref 529748 | J Med Chem. 2008 Nov 13;51(21):6725-39. Epub 2008 Oct 15.Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). | ||||
Ref 529748 | J Med Chem. 2008 Nov 13;51(21):6725-39. Epub 2008 Oct 15.Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). | ||||
Ref 529748 | J Med Chem. 2008 Nov 13;51(21):6725-39. Epub 2008 Oct 15.Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 530868 | Bioorg Med Chem. 2010 May 15;18(10):3494-505. Epub 2010 Mar 29.Novel estrone mimetics with high 17beta-HSD1 inhibitory activity. | ||||
Ref 530868 | Bioorg Med Chem. 2010 May 15;18(10):3494-505. Epub 2010 Mar 29.Novel estrone mimetics with high 17beta-HSD1 inhibitory activity. | ||||
Ref 530868 | Bioorg Med Chem. 2010 May 15;18(10):3494-505. Epub 2010 Mar 29.Novel estrone mimetics with high 17beta-HSD1 inhibitory activity. | ||||
Ref 530450 | J Med Chem. 2009 Nov 12;52(21):6724-43.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. | ||||
Ref 528033 | J Med Chem. 2006 Feb 23;49(4):1325-45.Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. | ||||
Ref 528033 | J Med Chem. 2006 Feb 23;49(4):1325-45.Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1. | ||||
Ref 529748 | J Med Chem. 2008 Nov 13;51(21):6725-39. Epub 2008 Oct 15.Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). |
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