2. Academic Validation
  3. Nortropinyl-arylsulfonylureas as novel, reversible inhibitors of human steroid sulfatase

Nortropinyl-arylsulfonylureas as novel, reversible inhibitors of human steroid sulfatase

  • Bioorg Med Chem Lett. 2003 Nov 3;13(21):3673-7. doi: 10.1016/j.bmcl.2003.08.019.
Peter Nussbaumer 1,  Dieter Geyl,  Amarylla Horvath,  Philipp Lehr,  Barbara Wolff,  Andreas Billich
Affiliations

Affiliation

  • 1 Novartis Research Institute Vienna, Brunnerstrasse 59, A-1235 Vienna, Austria. [email protected]
PMID: 14552755 DOI: 10.1016/j.bmcl.2003.08.019
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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