Evaluation of 3,4-dihydroquinazoline-2(1H)-thiones as inhibitors of alpha-MSH-induced melanin production in melanoma B16 cells.
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.
Thanigaimalai
P
P
College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, Republic of Korea.
Lee
Ki-Cheul
KC
Bang
Seong-Cheol
SC
Lee
Jee-Hyun
JH
Yun
Cheong-Yong
CY
Roh
Eunmiri
E
Hwang
Bang-Yeon
BY
Kim
Youngsoo
Y
Jung
Sang-Hun
SH
D000818:Animals; D045744:Cell Line, Tumor; D004353:Drug Evaluation, Preclinical; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008543:Melanins / Q000096:biosynthesis*; D008546:Melanoma, Experimental / Q000378:metabolism* / Q000473:pathology; D051379:Mice; D011799:Quinazolines / Q000494:pharmacology*; D017550:Spectroscopy, Fourier Transform Infrared; D000521:alpha-MSH / Q000037:antagonists & inhibitors* / Q000502:physiology
D008543:Melanins; D011799:Quinazolines; D000521:alpha-MSH