European journal of medicinal chemistry

Chemical synthesis and evaluation of 17α-alkylated derivatives of estradiol as inhibitors of steroid sulfatase

D Fournier, D Poirier

Index: Fournier, Diane; Poirier, Donald European Journal of Medicinal Chemistry, 2011 , vol. 46, # 9 p. 4227 - 4237

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Citation Number: 11

Abstract

Steroid sulfatase (STS) controls the levels of 3-hydroxysteroids available from circulating steroid sulfates in several normal and malignant tissues. This and the known involvement of active estrogens and androgens in diseases such as breast and prostate cancers thus make STS an interesting therapeutic target. Here we describe the chemical synthesis and characterization of an extended series of 17α-derivatives of estradiol (E2) using different ...