Pyrazole-based cathepsin S inhibitors with improved cellular potency (original) (raw)
2007, Bioorganic & Medicinal Chemistry Letters
High potency pyrazole-based noncovalent inhibitors of human cathepsin S (CatS) were developed by modification of the benzo-fused 5-membered ring heterocycles found in earlier series of CatS inhibitors. Although substitutions on this heterocyclic framework had a moderate impact on enzymatic potency, dramatic effects on cellular activity were observed. Optimization afforded indole-and benzothiophene-derived analogues that were high affinity CatS inhibitors (IC 50 = 20-40 nM) with good cellular potency (IC 50 = 30-340 nM).
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