Synthesis and Bioactivity of New Chalcone Derivatives as Potential Tyrosinase Activator Based on the Click Chemistry

被引：20

作者：

Niu, Chao ^{[1
,2
]}

Li, Gen ^{[1
,2
]}

Tuerxuntayi, Adila ^{[1
,2
]}

Aisa, Haji A. ^{[1
,2
]}

机构：

[1] Chinese Acad Sci, Key Lab Plant Resources & Chem Arid Zone, Urumqi 830011, Xinjiang, Peoples R China

[2] Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Urumqi 830011, Xinjiang, Peoples R China

来源：

CHINESE JOURNAL OF CHEMISTRY | 2015年 / 33卷 / 04期

基金：

中国国家自然科学基金;

关键词：

enzyme; chalcone; heterocycles; synthesis; structure-activity relationship; 8-METHOXYPSORALEN; INHIBITORS; PATHWAY;

D O I：

10.1002/cjoc.201400820

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A new series of (E)-1-(4-((1-benzyl-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-3-phenylprop-2-en-1-one 1a(4-((1-benzyl-1H-1,2,3-triazol-4-yl) methoxy)phenyl)-1-phenylprop-2-en-1-one 1b-15b were designed, synthesized based on click chemistry, and biologically evaluated for their activity on tyrosinase. The result showed that most of prepared compounds 1a-15a have potent activating effect on tyrosinase, especially for 3a, 8a-10a and 14a-15a. Among them, compounds 10a and 14a demonstrated the best activity with EC50=1.71 and 5.60 mu molL(-1) respectively, even better than the positive control 8-MOP (EC50=14.8 mu molL(-1)). Conversely, compounds 3b, 5b-6b, 9b-10b, and 15b induced enzymatic inhibition on tyrosinase.

引用

页码：486 / 494

页数：9

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