评价 3,4-二氢喹唑啉-2(1H)-硫酮类化合物对黑色素瘤 B16 细胞中 alpha-MSH 诱导的黑色素生成的抑制作用。
Evaluation of 3,4-dihydroquinazoline-2(1H)-thiones as inhibitors of alpha-MSH-induced melanin production in melanoma B16 cells.
机构信息
College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, Republic of Korea.
出版信息
Bioorg Med Chem. 2010 Feb 15;18(4):1555-62. doi: 10.1016/j.bmc.2010.01.005. Epub 2010 Jan 11.
Novel 3,4-dihydroquinazoline-2(1H)-thiones (QNTs) 1 were found to be potent inhibitors of alpha-MSH-induced melanin production. The effect of QNTs to inhibit melanin formation in B16 melanoma cells was screened in the presence of alpha-MSH. In defining the mechanism of activity, the effects on tyrosinase activity, on tyrosinase synthesis and on the depigmentation of melanin were evaluated. QNTs did not affect the catalytic activity of tyrosinase, but rather acted as an inhibitor of tyrosinase synthesis.
新型 3,4-二氢喹唑啉-2(1H)-硫酮（QNTs）1 被发现是α-MSH 诱导的黑色素生成的有效抑制剂。在α-MSH 存在的情况下，筛选 QNTs 抑制 B16 黑色素瘤细胞中黑色素形成的作用。在确定作用机制时，评估了对酪氨酸酶活性、酪氨酸酶合成和黑色素褪色的影响。QNTs 不影响酪氨酸酶的催化活性，而是作为酪氨酸酶合成的抑制剂。
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