Evaluation of 3,4-dihydroquinazoline-2(1H)-thiones as inhibitors of alpha-MSH-induced melanin production in melanoma B16 cells

P Thanigaimalai; Ki-Cheul Lee; Seong-Cheol Bang; Jee-Hyun Lee; Cheong-Yong Yun; Eunmiri Roh; Bang-Yeon Hwang; Youngsoo Kim; Sang-Hun Jung

doi:10.1016/j.bmc.2010.01.005

Evaluation of 3,4-dihydroquinazoline-2(1H)-thiones as inhibitors of alpha-MSH-induced melanin production in melanoma B16 cells

Bioorg Med Chem. 2010 Feb 15;18(4):1555-62. doi: 10.1016/j.bmc.2010.01.005. Epub 2010 Jan 11.

Authors

P Thanigaimalai¹, Ki-Cheul Lee, Seong-Cheol Bang, Jee-Hyun Lee, Cheong-Yong Yun, Eunmiri Roh, Bang-Yeon Hwang, Youngsoo Kim, Sang-Hun Jung

Affiliation

¹ College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, Republic of Korea.

PMID: 20097083
DOI: 10.1016/j.bmc.2010.01.005

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Cell Line, Tumor
Drug Evaluation, Preclinical
Magnetic Resonance Spectroscopy
Mass Spectrometry
Melanins / biosynthesis*
Melanoma, Experimental / metabolism*
Melanoma, Experimental / pathology
Mice
Quinazolines / pharmacology*
Spectroscopy, Fourier Transform Infrared
alpha-MSH / antagonists & inhibitors*
alpha-MSH / physiology

Substances

Melanins
Quinazolines
alpha-MSH