Synthesis and Biological Evaluation of Spiro-δ-lactones as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2)
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This article is published in Letters in Drug Design & Discovery.The article was published on 2011-05-31 and is currently open access. It has received 11 citations till now. The article focuses on the topics: Hydroxysteroid dehydrogenase.read more
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Journal ArticleDOI
Hydroxybenzothiazoles as new nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1).
Alessandro Spadaro,Matthias Negri,Sandrine Marchais-Oberwinkler,Emmanuel Bey,Martin Frotscher +4 more
TL;DR: A novel pharmacophore model was derived from crystallographic data and used for the virtual screening of a small library of compounds, resulting in the discovery of a novel class of 17β-HSD1 inhibitors bearing a benzothiazole-scaffold linked to a phenyl ring via keto- or amide-bridge.
Journal ArticleDOI
Inhibitors of 17β-hydroxysteroid dehydrogenase type 1, 2 and 14: Structures, biological activities and future challenges.
TL;DR: The present review gives a survey on the development of inhibitor classes as well as the structural formulas and biological properties of their most interesting representatives.
Journal ArticleDOI
Lead optimization of 17β-HSD1 inhibitors of the (hydroxyphenyl)naphthol sulfonamide type for the treatment of endometriosis.
Claudia Henn,Almuth Einspanier,Sandrine Marchais-Oberwinkler,Martin Frotscher,Rolf W. Hartmann +4 more
TL;DR: 4-indolylsulfonamide 30 is a highly active and selective human 17 β-HSD1 inhibitor, as well as a highly potent and selective inhibitor of 17β- HSD1 from Callithrix jacchus, which shows no affinity to the estrogen receptors α and β and good intracellular activity (T47D).
Journal ArticleDOI
Metabolic stability optimization and metabolite identification of 2,5-thiophene amide 17β-hydroxysteroid dehydrogenase type 2 inhibitors.
Emanuele M. Gargano,Enrico Perspicace,Nina Hanke,Angelo Carotti,Sandrine Marchais-Oberwinkler,Rolf W. Hartmann +5 more
TL;DR: A rational strategy to overcome the metabolic liability in the 2,5-thiophene amide class of 17β-HSD2 inhibitors is described, and the biological activity of the new inhibitors are described.
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Novel, potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors as potential therapeutics for osteoporosis with dual human and mouse activities.
Enrico Perspicace,Liliana Cozzoli,Emanuele M. Gargano,Nina Hanke,Angelo Carotti,Rolf W. Hartmann,Sandrine Marchais-Oberwinkler +6 more
TL;DR: The design, the synthesis and the biological evaluation of 24 new 17β-HSD2 inhibitors in the 5-substituted thiophene-2-carboxamide class are described and new structural insights into the active sites of the human and mouse enzymes were gained.
References
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Skeletal Effects of Estrogen
TL;DR: Estrogen appears to be the most important sex steroid in preventing osteoporosis in women and is the subject of this review.
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Androgens and bone
Dirk Vanderschueren,Liesbeth Vandenput,Steven Boonen,Marie K. Lindberg,Roger Bouillon,Claes Ohlsson +5 more
TL;DR: Observations in androgen-resistant animals clearly demonstrated that the sexual dimorphism of bone depends on the presence of a functional androgen receptor, and optimal peak bone mass seems related to an appropriately timed androgen secretion.
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Hip fracture and the use of estrogens in postmenopausal women. The Framingham Study.
TL;DR: Taking estrogen within four years of menopause also protected against hip fracture, and the adjusted relative risk in women who had taken estrogens within the previous two years was further reduced.
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The role of 17 beta-hydroxysteroid dehydrogenases.
TL;DR: 17 beta-hydroxysteroid dehydrogenases reveal a remarkable multifunctionality being able to modulate concentrations not only of steroids but as well of fatty and bile acids.
Journal ArticleDOI
Integrated view on 17beta-hydroxysteroid dehydrogenases.
Gabriele Moeller,Jerzy Adamski +1 more
TL;DR: In this article, metabolic activities of 17β-HSDs are compared, their interplay with endogenous substrates summarised, and interlacing pathways depicted, and strategies on deciphering the physiological role of 17beta-HSD and the genetic predisposition for associated diseases are presented.