doi: 10.1016/j.bmc.2009.12.044.
Epub 2009 Dec 22.
Inhibitory effect of novel tetrahydropyrimidine-2(1H)-thiones on melanogenesis
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- PMID: 20044259
- DOI: 10.1016/j.bmc.2009.12.044
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Inhibitory effect of novel tetrahydropyrimidine-2(1H)-thiones on melanogenesis
Bioorg Med Chem.
2010 Feb.
Abstract
The series of imidazoldine-2-thiones 2 and tetrahydropyrimidine-2-thiones 3 were discovered as inhibitor of alpha-MSH-induced melanin production in melanoma B16 cells. The primary bioassay showed that 1-(4-ethylbenzyl)-tetrahydropyrimidine-2(1H)-thione 3e (>100% inhibition at 10 microM, IC(50)=1.2 microM) and 1-(4-tert-butylbenzyl)-tetrahydropyrimidine-2(1H)-thione 3f (>100% inhibition at 10 microM, IC(50)=0.76 microM) exhibited potent inhibitory effect against alpha-MSH-induced melanin production. Compounds 3 inhibit the biosynthesis of tyrosinase without affecting its catalytic activity in melanogenesis.
Copyright (c) 2010 Elsevier Ltd. All rights reserved.
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