期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 3, 页码 1135-1142出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.12.044
关键词
Tetrahydropyrimidine-2(1H)-thione; alpha-MSH-induced melanin production; Hypopimenting; Melanogenesis
资金
- National Research Foundation of Korea [R01-2007000-20099-0]
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 mu M, IC50 = 1.2 mu M) and 1-(4-tert-butylbenzyl)-tetrahydropyrimidine-2(1H)-thione 3f (> 100% inhibition at 10 mu M, IC50 = 0.76 mu M) exhibited potent inhibitory effect against alpha-MSH-induced melanin production. Compounds 3 inhibit the biosynthesis of tyrosinase without affecting its catalytic activity in melanogenesis. (C) 2010 Elsevier Ltd. All rights reserved.
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