Inhibitory effect of novel tetrahydropyrimidine-2(1H)-thiones on melanogenesis |
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| Authors: | P Thanigaimalai Ki-Cheul Lee Seong-Cheol Bang Jee-Hyun Lee Cheong-Yong Yun Eunmiri Roh Bang-Yeon Hwang Youngsoo Kim Sang-Hun Jung |
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| Institution: | 1. College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, Republic of Korea;2. College of Pharmacy, Chungbuk National University, Cheongu 361-763, Republic of Korea |
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| Abstract: | The series of imidazoldine-2-thiones 2 and tetrahydropyrimidine-2-thiones 3 were discovered as inhibitor of α-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 μM, IC50 = 1.2 μM) and 1-(4-tert-butylbenzyl)-tetrahydropyrimidine-2(1H)-thione 3f (>100% inhibition at 10 μM, IC50 = 0.76 μM) exhibited potent inhibitory effect against α-MSH-induced melanin production. Compounds 3 inhibit the biosynthesis of tyrosinase without affecting its catalytic activity in melanogenesis. |
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