title: Tetraketones: a new class of tyrosinase inhibitors.
abstract: 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.
authors.affiliation: H.E.J. Research Institute of Chemistry, International Center for Chemical Sciences, University of Karachi, Karachi 75270, Pakistan. hassaan2@super.net.pk
authors.forename: Khalid Mohammed
authors.initials: KM
authors.lastname: Khan
authors.forename: Ghulam Murtaza
authors.initials: GM
authors.lastname: Maharvi
authors.forename: Mahmud Tareq Hassan
authors.initials: MT
authors.lastname: Khan
authors.forename: Ahson
authors.initials: A
authors.lastname: Jabbar Shaikh
authors.forename: Shahnaz
authors.initials: S
authors.lastname: Perveen
authors.forename: Saeedan
authors.initials: S
authors.lastname: Begum
authors.forename: Mohammad Iqbal
authors.initials: MI
authors.lastname: Choudhary
mesh_terms: D004791:Enzyme Inhibitors / Q000494:pharmacology*; D007659:Ketones / Q000494:pharmacology*; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors*; D013057:Spectrum Analysis / Q000379:methods
chemical_list: D004791:Enzyme Inhibitors; D007659:Ketones; D014442:Monophenol Monooxygenase