| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10594131 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
A non-estrogenic inhibitor of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) was designed based on a modified 3-hydroxy-estra-1,3,5(10)-triene core having an additional five-member lactone ring and a benzamide group. The inhibitor was synthesized, fully characterized and tested for its ability to inhibit the enzyme activity. Estrogenicity was also investigated and tested on estrogen-dependent T-47D cell line. Interestingly, this steroid derivative showed inhibitory potency towards 17β-HSD1 and did not present residual unwanted estrogenic activity.
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Authors
Ãtienne Ouellet, Diana Ayan, Donald Poirier,