N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase

P Lehr, A Billich, B Wolff, P Nussbaumer

Index: Lehr, Philipp; Billich, Andreas; Wolff, Barbara; Nussbaumer, Peter Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 4 p. 1235 - 1238

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Citation Number: 15

Abstract

Steroid sulfatase (STS) is an attractive target for a range of oestrogen-and androgen- dependent diseases. In search of novel chemotypes of STS inhibitors, we had previously identified nortropinyl–arylsulfonylureas 1; however, while these compounds were good inhibitors of purified STS (lowest Ki= 76nM), they showed only weak inhibition of STS activity in cells (lowest IC50 around 2μM). Extended structure–activity relationship studies ...