Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 21, Issue 11, Pages 2975-2987Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.03.062
Keywords
Cysteine protease inhibitor; Cathepsin inhibitor; Sulfonyloxiranes; Cancer metastasis; Cell migration
Funding
- PSC-CUNY Research Award Program
- Queensborough Community College (QCC)/Queens College NSF-STEP
- NIH
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Cysteine cathepsins are an important class of enzymes that coordinate a variety of important cellular processes, and are implicated in various types of human diseases. However, small molecule inhibitors that are cell-permeable and non-peptidyl in nature are scarcely available. Herein the synthesis and development of sulfonyloxiranes as covalent inhibitors of cysteine cathepsins are reported. From a library of compounds, compound 5 is identified as a selective inhibitor of cysteine cathepsins. Live cell imaging and immunocytochemistry of metastatic human breast carcinoma MDA-MB-231 cells document the efficacy of compound 5 in inhibiting cysteine cathepsin activity in living cells. A cell-motility assay demonstrates that compound 5 is effective in mitigating the cell-migratory potential of highly metastatic breast carcinoma MDA-MB-231 cells. (C) 2013 Elsevier Ltd. All rights reserved.
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