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

2.50
Hdl Handle:
http://hdl.handle.net/10033/615613
Title:
17β-Hydroxysteroid Dehydrogenase Type 2 Inhibition: Discovery of Selective and Metabolically Stable Compounds Inhibiting Both the Human Enzyme and Its Murine Ortholog.
Authors:
Gargano, Emanuele M; Allegretta, Giuseppe; Perspicace, Enrico; Carotti, Angelo; Van Koppen, Chris; Frotscher, Martin; Marchais-Oberwinkler, Sandrine; Hartmann, Rolf W
Abstract:
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 toward h17β-HSD1, m17β-HSD1 and estrogen receptors α and β as well as appropriate physicochemical properties for oral bioavailability. These properties make it eligible for pre-clinical animal studies, prior to human studies.
Affiliation:
Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS),Saarland 9 University, 66123 Saarbrücken, Germany.
Citation:
17β-Hydroxysteroid Dehydrogenase Type 2 Inhibition: Discovery of Selective and Metabolically Stable Compounds Inhibiting Both the Human Enzyme and Its Murine Ortholog. 2015, 10 (7):e0134754 PLoS ONE
Journal:
PloS one
Issue Date:
2015
URI:
http://hdl.handle.net/10033/615613
DOI:
10.1371/journal.pone.0134754
PubMed ID:
26230928
Type:
Article
Language:
en
ISSN:
1932-6203
Appears in Collections:
publications of the department drug design and optimization (HIPS]DDOP)

Full metadata record

DC FieldValue Language
dc.contributor.authorGargano, Emanuele Men
dc.contributor.authorAllegretta, Giuseppeen
dc.contributor.authorPerspicace, Enricoen
dc.contributor.authorCarotti, Angeloen
dc.contributor.authorVan Koppen, Chrisen
dc.contributor.authorFrotscher, Martinen
dc.contributor.authorMarchais-Oberwinkler, Sandrineen
dc.contributor.authorHartmann, Rolf Wen
dc.date.accessioned2016-07-06T09:39:32Z-
dc.date.available2016-07-06T09:39:32Z-
dc.date.issued2015-
dc.identifier.citation17β-Hydroxysteroid Dehydrogenase Type 2 Inhibition: Discovery of Selective and Metabolically Stable Compounds Inhibiting Both the Human Enzyme and Its Murine Ortholog. 2015, 10 (7):e0134754 PLoS ONEen
dc.identifier.issn1932-6203-
dc.identifier.pmid26230928-
dc.identifier.doi10.1371/journal.pone.0134754-
dc.identifier.urihttp://hdl.handle.net/10033/615613-
dc.description.abstractDesign 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 toward h17β-HSD1, m17β-HSD1 and estrogen receptors α and β as well as appropriate physicochemical properties for oral bioavailability. These properties make it eligible for pre-clinical animal studies, prior to human studies.en
dc.language.isoenen
dc.rights.urihttp://creativecommons.org/licenses/by-nc-sa/4.0/*
dc.subject.meshAnimalsen
dc.subject.meshCell Line, Tumoren
dc.subject.meshEnzyme Inhibitorsen
dc.subject.meshEstradiol Dehydrogenasesen
dc.subject.meshHumansen
dc.subject.meshMiceen
dc.subject.meshStructure-Activity Relationshipen
dc.title17β-Hydroxysteroid Dehydrogenase Type 2 Inhibition: Discovery of Selective and Metabolically Stable Compounds Inhibiting Both the Human Enzyme and Its Murine Ortholog.en
dc.typeArticleen
dc.contributor.departmentHelmholtz-Institute for Pharmaceutical Research Saarland (HIPS),Saarland 9 University, 66123 Saarbrücken, Germany.en
dc.identifier.journalPloS oneen

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