Author/Authors :
P. Thanigaimalai، نويسنده , , Ki-Cheul Lee، نويسنده , , Seong-Cheol Bang، نويسنده , , Jeehyun Lee، نويسنده , , Cheong-Yong Yun، نويسنده , , Eunmiri Roh، نويسنده , , Bang Yeon Hwang، نويسنده , , Youngsoo Kim، نويسنده , , Sang-Hun Jung، نويسنده ,
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.
Keywords :
?-MSH-induced melanin production , Hypopimenting , Tetrahydropyrimidine-2(1H)-thione , Melanogenesis
