Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 7, Pages 2491-2494Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.02.043
Keywords
beta-lactone; thioesterase domain; anticancer; tandem Mukaiayama aldol-lactonization
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Funding
- NCI NIH HHS [CA10658] Funding Source: Medline
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beta-Lactam derivatives of orlistat were prepared and their inhibitory activities toward the thioesterase domain of fatty acid synthase (FAS-TE) were evaluated using a recombinant form of the enzyme. While in general these derivatives showed lower potency compared to beta-lactones, a reasonably potent, lead compound (-)-9 (IC50 = 8.6 mu M) was discovered that suggests that this class of compounds should be evaluated further. (C) 2008 Published by Elsevier Ltd.
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