| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1368782 | Bioorganic & Medicinal Chemistry Letters | 2016 | 4 Pages |
Abstract
Four different classes of new 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors were synthesized, in order to lower the cytotoxicity exhibited by the lead compound A, via disrupting the linearity and the aromaticity of the biphenyl moiety. Compounds 3, 4, 7a and 8 displayed comparable or better inhibitory activity and selectivity, as well as a lower cytotoxic effect, compared to the reference compound A. The best compound 4 (IC50 = 160 nM, selectivity factor = 168, LD50 ≈ 25 μM) turned out as new lead compound for inhibition of 17β-HSD2.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Emanuele Marco Gargano, Enrico Perspicace, Angelo Carotti, Sandrine Marchais-Oberwinkler, Rolf W. Hartmann,