17β-Hydroxysteroid Dehydrogenase Type 2 Inhibition: Discovery of Selective and Metabolically Stable Compounds Inhibiting Both the Human Enzyme and Its Murine Ortholog

Design and synthesis of a new class of inhibitors for the treatment of osteoporosis and its comparative h17β-HSD2 and m17β-HSD2 SAR study are described. 17a is the first compound to show strong inhibition of both h17β-HSD2 and m17β-HSD2, intracellular activity, metabolic stability, selectivity towar...

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Detalles Bibliográficos
Autores principales: Gargano, Emanuele M., Allegretta, Giuseppe, Perspicace, Enrico, Carotti, Angelo, Van Koppen, Chris, Frotscher, Martin, Marchais-Oberwinkler, Sandrine, Hartmann, Rolf W.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2015
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4521925/
https://www.ncbi.nlm.nih.gov/pubmed/26230928
http://dx.doi.org/10.1371/journal.pone.0134754

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4521925/
https://www.ncbi.nlm.nih.gov/pubmed/26230928
http://dx.doi.org/10.1371/journal.pone.0134754

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