N-Acyl Arylsulfonamides as Novel, Reversible Inhibitors of Human Steroid Sulfatase

    December 2004 in “ Bioorganic & Medicinal Chemistry Letters ”
    Philipp Lehr, Andreas Billich, Barbara Wolff, Peter Nussbaumer
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    TLDR Scientists found new, better-working inhibitors for a hormone-related enzyme.
    The document detailed the identification of N-acyl arylsulfonamides as new, reversible inhibitors of human steroid sulfatase (STS), which is significant for treating hormone-dependent diseases. Previous inhibitors were less effective in cellular environments. Through research, the scientists created N-acyl arylsulfonamides with better cellular efficacy, with the most effective compound showing an IC50 value of 270 nM. These inhibitors were competitive and lacked oestrogenic activity in vitro. The compound named 4f was particularly potent, with an IC50 of 26 nM against STS in its purified form and 270 nM in cellular assays, outperforming earlier inhibitors. The study concluded that N-acyl arylsulfonamides are promising candidates for further development and possible clinical testing due to their improved cellular potency.
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