Design, synthesis and molecular simulation studies of dihydrostilbene derivatives as potent tyrosinase inhibitors

被引：36
|
作者：
Vontzalidou, Argyro [1 ]
Zoidis, Grigoris [1 ,2 ]
Chaita, Eliza [1 ]
Makropoulou, Maria [1 ]
Aligiannis, Nektarios [1 ]
Lambrinidis, George [2 ]
Mikros, Emmanuel [2 ]
Skaltsounis, Alexios-Leandros [1 ]
机构：
[1] Univ Athens, Fac Pharm, Dept Pharmacognosy & Nat Prod Chem, GR-15771 Athens, Greece
[2] Univ Athens, Fac Pharm, Dept Pharmaceut Chem, GR-15771 Athens, Greece
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 17期
关键词：
Deoxybenzoins; Dihydrostilbenes; Tyrosinase inhibitors; Kojic acid; Gallic acid; Molecular simulations; IDENTIFICATION; DOPAMINE;
D O I：
10.1016/j.bmcl.2012.07.029
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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 (IC50 = 8.44 mu M, more potent than kojic acid). (C) 2012 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5523 / 5526
页数：4
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