Structure-activity relationship for aryl and heteroaryl boronic acid inhibitors of hormone-sensitive lipase
- PMID: 15727879
- DOI: 10.1016/j.bmc.2004.12.042
Structure-activity relationship for aryl and heteroaryl boronic acid inhibitors of hormone-sensitive lipase
Abstract
A range of aryl and heteroaryl boronic acids were tested for their in vitro hormone-sensitive lipase inhibitory properties. (2-Benzyloxy-5-fluorophenyl)boronic acid, (2-benzyloxy-5-chlorophenyl)boronic acid and 5-bromothiophene-2-boronic acid were found to be the most potent HSL inhibitors with IC(50) values of 140, 17 and 350 nM, respectively.
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