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

Lehr, Philipp and Billich, Andreas and Wolff-Winiski, Barbara and Nussbaumer, Peter (2005) N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase. Bioorganic & Medicinal Chemistry Letters, 15 (4). pp. 1235-1238. ISSN 0960-894X

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 K(i)=76 nM), they showed only weak inhibition of STS activity in cells (lowest IC(50) around 2 microM). Extended structure-activity relationship studies involving modification of the phenylacetyl side chain and replacement of the nortropine element by simpler scaffolds led to the discovery of N-acyl arylsulfonamides, more specifically N-(Boc-piperidine-4-carbonyl)-benzenesulfonamides, as STS inhibitors, some of which exhibit improved cellular potency (best IC(50)=270 nM).

Item Type: Article
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Date Deposited: 14 Dec 2009 13:56
Last Modified: 31 Jan 2013 01:10
URI: https://oak.novartis.com/id/eprint/671

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