A convenient synthesis of a selective gelatinase inhibitor as an antimetastatic agent |
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Authors: | Lim In Taek Brown Stephen Mobashery Shahriar |
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Institution: | Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, Indiana 46556, USA. |
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Abstract: | Compound 1, 2-(4-phenoxyphenylsulfonylmethyl)thiirane, is a potent and selective inhibitor for human gelatinases (J. Am. Chem. Soc. 2000, 122, 6799-6800), enzymes implicated in a number of diseases, including cancer. This compound is showing excellent promise in animal trials in a number of disease models. Large quantities of this compound were necessary for these studies. A convenient four-step synthetic route for compound 1 is described herein. The synthesis is amenable to scale-up to tens of grams and gives an overall yield of 57% for this important compound. |
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