title: Design, synthesis and molecular simulation studies of dihydrostilbene derivatives as potent tyrosinase inhibitors.
abstract: The synthesis, molecular modeling and biological evaluation of substituted deoxybenzoins and optimized dihydrostilbenes are reported. Preliminary structure-activity relationship data were elucidated and lead compounds suitable for further optimization were discovered. Dihydrostilbene 7 is a particularly potent inhibitor (IC(50)=8.44 μM, more potent than kojic acid).
authors: Faculty of Pharmacy, Department of Pharmacognosy and Natural Products Chemistry, University of Athens, Panepistimiopolis Zografou, GR-15771 Athens, Greece.
authors: Argyro
authors: A
authors: Vontzalidou
authors: Grigoris
authors: G
authors: Zoidis
authors: Eliza
authors: E
authors: Chaita
authors: Maria
authors: M
authors: Makropoulou
authors: Nektarios
authors: N
authors: Aligiannis
authors: George
authors: G
authors: Lambrinidis
authors: Emmanuel
authors: E
authors: Mikros
authors: Alexios-Leandros
authors: AL
authors: Skaltsounis
mesh_terms: D001419:Bacteria / Q000201:enzymology; D001573:Benzoin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D005658:Fungi / Q000201:enzymology; D062105:Molecular Docking Simulation; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011753:Pyrones / Q000737:chemistry / Q000494:pharmacology; D013267:Stilbenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D000081014:Dihydrostilbenoids
chemical_list: D001573:Benzoin; D004791:Enzyme Inhibitors; D014442:Monophenol Monooxygenase; D011753:Pyrones; D013267:Stilbenes; C038546:1,2-dihydrostilbene; D000081014:Dihydrostilbenoids; C011890:kojic acid; C492807:deoxybenzoin