Ontology highlight
ABSTRACT:
SUBMITTER: Gargano EM
PROVIDER: S-EPMC4521925 | biostudies-literature | 2015
REPOSITORIES: biostudies-literature
Gargano Emanuele M EM Allegretta Giuseppe G Perspicace Enrico E Carotti Angelo A Van Koppen Chris C Frotscher Martin M Marchais-Oberwinkler Sandrine S Hartmann Rolf W RW
PloS one 20150731 7
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, pri ...[more]