Author: Kishore Kumar, G.D.; Chavarria, Gustavo E.; Charlton-Sevcik, Amanda K.; Arispe, Wara M.; MacDonough, Matthew T.; Strecker, Tracy E.; Chen, Shen-En; Siim, Bronwyn G.; Chaplin, David J.; Trawick, Mary Lynn; Pinney, Kevin G.
Title: Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors Cord-id: efu1tiky Document date: 2010_2_15
ID: efu1tiky
Snippet: A small library of 36 functionalized benzophenone thiosemicarbazone analogs has been prepared by chemical synthesis and evaluated for their ability to inhibit the cysteine proteases cathepsin L and cathepsin B. Inhibitors of cathepsins L and B have the potential to limit or arrest cancer metastasis. The six most active inhibitors of cathepsin L (IC(50) < 85 nM) in this series incorporate a meta-bromo substituent in one aryl ring along with a variety of functional groups in the second aryl ring.
Document: A small library of 36 functionalized benzophenone thiosemicarbazone analogs has been prepared by chemical synthesis and evaluated for their ability to inhibit the cysteine proteases cathepsin L and cathepsin B. Inhibitors of cathepsins L and B have the potential to limit or arrest cancer metastasis. The six most active inhibitors of cathepsin L (IC(50) < 85 nM) in this series incorporate a meta-bromo substituent in one aryl ring along with a variety of functional groups in the second aryl ring. These six analogs are selective for their inhibition of cathepsin L versus cathepsin B (IC(50) > 10,000 nM). The most active analog in the series, 3-bromophenyl-2′-fluorophenyl thiosemicarbazone 1, also efficiently inhibits cell invasion of the DU-145 human prostate cancer cell line.
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