Design, synthesis and molecular simulation studies of dihydrostilbene derivatives as potent tyrosinase inhibitors.

Bioorg Med Chem Lett

Faculty of Pharmacy, Department of Pharmacognosy and Natural Products Chemistry, University of Athens, Panepistimiopolis Zografou, GR-15771 Athens, Greece.

Published: September 2012

The synthesis, molecular modeling and biological evaluation of substituted deoxybenzoins and optimized dihydrostilbenes are reported. Preliminary structure-activity relationship data were elucidated and lead compounds suitable for further optimization were discovered. Dihydrostilbene 7 is a particularly potent inhibitor (IC(50)=8.44 μM, more potent than kojic acid).

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http://dx.doi.org/10.1016/j.bmcl.2012.07.029DOI Listing

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