Tetraketones: a new class of tyrosinase inhibitors.
Twenty-eight tetraketones (1-28) with variable substituents at C-7 were synthesized and evaluated as tyrosinase inhibitors. Remarkably compounds 25 (IC(50)=2.06 microM), 11 (IC(50)=2.09 microM), 15 (IC(50)=2.61 microM), and 27 (IC(50)=3.19 microM) were found to be the most active compounds of the series, even better than both standards kojic acid (IC(50)=16.67 microM) and L-mimosine (IC(50)=3.68 microM). This study may lead to the discovery of therapeutically potent agents against clinically very important dermatological disorders including hyperpigmentation as well as skin melanoma.
Khan
Khalid Mohammed
KM
H.E.J. Research Institute of Chemistry, International Center for Chemical Sciences, University of Karachi, Karachi 75270, Pakistan. hassaan2@super.net.pk
Maharvi
Ghulam Murtaza
GM
Khan
Mahmud Tareq Hassan
MT
Jabbar Shaikh
Ahson
A
Perveen
Shahnaz
S
Begum
Saeedan
S
Choudhary
Mohammad Iqbal
MI
D004791:Enzyme Inhibitors / Q000494:pharmacology*; D007659:Ketones / Q000494:pharmacology*; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors*; D013057:Spectrum Analysis / Q000379:methods
D004791:Enzyme Inhibitors; D007659:Ketones; D014442:Monophenol Monooxygenase