College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, Republic of Korea.
Bioorg Med Chem. 2010 Feb;18(3):1135-42. doi: 10.1016/j.bmc.2009.12.044. Epub 2009 Dec 22.
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.
一系列咪唑并[2,1-b]噻唑-2-硫酮 2 和四氢嘧啶-2-硫酮 3 被发现是黑色素瘤 B16 细胞中α-MSH 诱导的黑色素生成的抑制剂。初步生物测定表明，1-(4-乙基苄基)-四氢嘧啶-2(1H)-硫酮 3e（在 10 μM 时抑制率超过 100%，IC50=1.2 μM）和 1-(4-叔丁基苄基)-四氢嘧啶-2(1H)-硫酮 3f（在 10 μM 时抑制率超过 100%，IC50=0.76 μM）对α-MSH 诱导的黑色素生成具有很强的抑制作用。化合物 3 抑制酪氨酸酶的生物合成，而不影响其在黑色素生成中的催化活性。
