Nortropinyl-arylsulfonylureas as novel, reversible inhibitors of human steroid sulfatase |
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Authors: | Nussbaumer Peter Geyl Dieter Horvath Amarylla Lehr Philipp Wolff Barbara Billich Andreas |
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Affiliation: | Novartis Research Institute Vienna, Brunnerstrasse 59, A-1235 Vienna, Austria. peter.nussbaumer@pharma.novartis.com |
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Abstract: | Steroid sulfatase (STS) has emerged as an attractive target for a range of estrogen- and androgen-dependent diseases. Searching for novel chemotypes as STS inhibitors, we identified nortropinyl-arylsulfonylurea 3 as a hit from high-throughput screening. A series of analogues was prepared in order to explore the essential structural elements for STS inhibition, and first structure-activity relationships were established. Mechanistic investigations revealed that the compounds are reversible, competitive inhibitors of STS. |
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