• Kishore KumarG DGDDepartment of Chemistry and Biochemistry, Baylor University, One Bear Place #97348, Waco, TX 76798-7348, USA., Gustavo E Chavarria, Amanda K Charlton-Sevcik, Wara M Arispe, Matthew T Macdonough, Tracy E Strecker, Shen-En Chen, Bronwyn G Siim, David J Chaplin, Mary Lynn Trawick, and Kevin G Pinney.
• Department of Chemistry and Biochemistry, Baylor University, One Bear Place #97348, Waco, TX 76798-7348, USA.
• Bioorg. Med. Chem. Lett. 2010 Feb 15; 20 (4): 1415-9.

AbstractA 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 (IC50<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 (IC50>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.Copyright 2010 Elsevier Ltd. All rights reserved.

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