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Synthesis and Bioactivity of New Chalcone Derivatives as Potential Tyrosinase Activator Based on the Click Chemistry
Niu, C (Niu, Chao); Li, G (Li, Gen); Tuerxuntayi, A (Tuerxuntayi, Adila); Aisa, HA (Aisa, Haji A.); Aisa, HA
2015
Source PublicationCHINESE JOURNAL OF CHEMISTRY
Volume33Issue:4Pages:486-494
Abstract

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.

KeywordEnzyme Chalcone Heterocycles Synthesis Structure-activity Relationship
DOI10.1002/cjoc.201400820
Indexed BySCI
WOS IDWOS:000352861200015
Citation statistics
Cited Times:14[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.xjipc.cas.cn/handle/365002/5165
Collection省部共建新疆特有药用资源利用重点实验室
Corresponding AuthorAisa, HA
Affiliation1.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
Recommended Citation
GB/T 7714
Niu, C ,Li, G ,Tuerxuntayi, A ,et al. Synthesis and Bioactivity of New Chalcone Derivatives as Potential Tyrosinase Activator Based on the Click Chemistry[J]. CHINESE JOURNAL OF CHEMISTRY,2015,33(4):486-494.
APA Niu, C ,Li, G ,Tuerxuntayi, A ,Aisa, HA ,&Aisa, HA.(2015).Synthesis and Bioactivity of New Chalcone Derivatives as Potential Tyrosinase Activator Based on the Click Chemistry.CHINESE JOURNAL OF CHEMISTRY,33(4),486-494.
MLA Niu, C ,et al."Synthesis and Bioactivity of New Chalcone Derivatives as Potential Tyrosinase Activator Based on the Click Chemistry".CHINESE JOURNAL OF CHEMISTRY 33.4(2015):486-494.
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