Estradiol dimers as a new class of steroid sulfatase reversible inhibitors

Bioorganic & Medicinal Chemistry Letters
Diane Fournier, Donald Poirier

Abstract

A series of estradiol dimers was synthesized or selected from compounds available in our laboratory and tested for inhibition against steroid sulfatase. Dimers linked by their C17 position, compounds 7 and 8, showed inhibitory potency similar (56% and 54% at 1 microM) to that of our best previously reported reversible inhibitor EM-690 (62% at 1 microM). Docking experiment seems to indicate that C17-C17 dimers bind in a similar way to EM-690 whereas C16-O3 and C16-C16 dimers bind in an upside-down position.

References

Jun 3, 2004·Biochimica Et Biophysica Acta·Jorge R Pasqualini
Feb 7, 2006·Mini Reviews in Medicinal Chemistry·Donald Poirier, René Maltais
Jun 15, 2007·Cellular and Molecular Life Sciences : CMLS·D Ghosh
Oct 16, 2007·Breast Cancer Research and Treatment·Ashok SubramanianKefah Mokbel

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Citations

Apr 5, 2011·Steroids·René Maltais, Donald Poirier
Mar 15, 2016·European Journal of Medicinal Chemistry·Ramanpreet ShahNirmal Singh
Jun 14, 2014·The Journal of Steroid Biochemistry and Molecular Biology·Natalija M KrstićDušan M Sladić
Feb 9, 2013·The Journal of Steroid Biochemistry and Molecular Biology·Yaser A Mostafa, Scott D Taylor
Mar 17, 2010·Chemistry & Biodiversity·Keguang ChengJuan Xie

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