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  • Title: Tetraketones: a new class of tyrosinase inhibitors.
    Author: Khan KM, Maharvi GM, Khan MT, Jabbar Shaikh A, Perveen S, Begum S, Choudhary MI.
    Journal: Bioorg Med Chem; 2006 Jan 15; 14(2):344-51. PubMed ID: 16198580.
    Abstract:
    Twenty-eight tetraketones (1-28) with variable substituents at C-7 were synthesized and evaluated as tyrosinase inhibitors. Remarkably compounds 25 (IC(50)=2.06 microM), 11 (IC(50)=2.09 microM), 15 (IC(50)=2.61 microM), and 27 (IC(50)=3.19 microM) were found to be the most active compounds of the series, even better than both standards kojic acid (IC(50)=16.67 microM) and L-mimosine (IC(50)=3.68 microM). This study may lead to the discovery of therapeutically potent agents against clinically very important dermatological disorders including hyperpigmentation as well as skin melanoma.
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