Design and discovery of tyrosinase inhibitors based on a coumarin scaffold

M. J. Matos; C. Varela; S. Vilar

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Design and discovery of tyrosinase inhibitors based on a coumarin scaffold

机译：基于香豆素脚手架的酪氨酸酶抑制剂的设计与发现

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In this manuscript we report the synthesis, pharmacological evaluation and docking studies of a selected series of 3-aryl and 3-heteroarylcoumarins with the aim of finding structural features for the tyrosinase inhibitory activity. The synthesized compounds were evaluated as mushroom tyrosinase inhibitors. Compound 12b showed the lowest IC_(50) (0.19 mM) of the series, being approximately 100 times more active than kojic acid, used as a reference compound. The kinetic studies of tyrosinase inhibition revealed that 12b acts as a competitive inhibitor of mushroom tyrosinase with L-DOPA as the substrate. Furthermore, the absence of cytotoxicity in B16F10 melanoma cells was determined for this compound. The antioxidant profile of all the derivatives was evaluated by measuring radical scavenging capacity (ABTS and DPPH assays). Docking experiments were carried out on mushroom tyrosinase structures to better understand the structure-activity relationships.

机译：在该手稿中，我们报告了选定的3-芳基和3-杂芳基的草林的合成，药理评估和对接研究，目的是寻找酪氨酸酶抑制活性的结构特征。将合成的化合物评价为蘑菇酪氨酸酶抑制剂。化合物12b显示该系列的最低IC_（50）（0.19mm），其比Kojic酸更高的100倍，用作参考化合物。酪氨酸酶抑制的动力学研究表明，12B作为具有L-DOPA作为基质的蘑菇酪氨酸酶的竞争抑制剂。此外，测定B16F10黑色素瘤细胞中细胞毒性的不存在该化合物。通过测量自由基清除能力（ABTS和DPPH测定）来评估所有衍生物的抗氧化谱。对接实验在蘑菇酪氨酸酶结构上进行，以更好地了解结构 - 活性关系。

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《RSC Advances》 |2015年第114期|共9页
作者
M. J. Matos; C. Varela; S. Vilar;
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CIQUP/Department of Chemistry and Biochemistry Faculty of Sciences University of Porto 4169-007 Porto Portugal.;

CNC-IBILI Pharmaceutical Chemistry Group Faculty of Pharmacy University of Coimbra 3000-548 Coimbra Portugal;

Department of Organic Chemistry Faculty of Pharmacy University of Santiago de Compostela 15782 Santiago de Compostela Spain;

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1. Design and discovery of tyrosinase inhibitors based on a coumarin scaffold [J] . M. J. Matos, C. Varela, S. Vilar RSC Advances . 2015,第114期

机译：基于香豆素脚手架的酪氨酸酶抑制剂的设计与发现
2. Structure-Based Design and Synthesis of an Isozyme-Selective MTHFD2 Inhibitor with a Tricyclic Coumarin Scaffold [J] . Kawai Junya, Ota Masahiro, Ohki Hitoshi, ACS medicinal chemistry letters . 2019,第6期

机译：基于结构的单性选择性MTHFD2抑制剂的结构和合成，具有三环香豆素脚手架
3. Discovery of novel inhibitors of Aurora kinases with indazole scaffold: In silico fragment-based and knowledge-based drug design [J] . Chang Chun-Feng, Lin Wen-Hsing, Ke Yi-Yu, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2016,第Null期

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5. Computational ligand-based cns therapeutic design: The search for novel-scaffold norepinephrine transporter inhibitors. [D] . Chaly, Anna. 2012

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6. Discovery of novel coumarin derivatives as potent and orally bioavailable BRD4 inhibitors based on scaffold hopping [O] . Zhimin Zhang, Lili Gu, Beibei Wang, 2019

机译：基于支架跳跃的新型香豆素衍生物作为有效和口服生物利用的BRD4抑制剂的发现
7. Structure-Based Design and Synthesis of an Isozyme-Selective MTHFD2 Inhibitor with a Tricyclic Coumarin Scaffold [O] . Junya Kawai, Masahiro Ota, Hitoshi Ohki, 2019

机译：基于结构的设计和合成同工酶选择性MTHFD2抑制剂，三环香豆素脚手架

Design and discovery of tyrosinase inhibitors based on a coumarin scaffold

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