Rational design, synthesis and structure-activity relationships of 4-alkoxy- and 4-acyloxy-phenylethylenethiosemicarbazone analogues as novel tyrosinase inhibitors
文献类型：期刊论文
| 作者 | You, Ao1; Zhou, Jie1,2; Song, Senchuan1; Zhu, Guoxun1; Song, Huacan1; Yi, Wei1,2 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2015-03-01 |
| 卷号 | 23期号:5页码:924-931 |
| 关键词 | 4-Alkoxy- and 4-acyloxy-phenylethylenethiosemicarbazone analogues Tyrosinase inhibitor SARs Inhibition mechanism Inhibitory kinetics |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2015.01.024 |
| 文献子类 | Article |
| 英文摘要 | In continuing our program aimed to search for potent compounds as highly efficient tyrosinase inhibitors, here a series of novel 4-alkoxy- and 4-acyloxy-phenylethylenethiosemicarbazone analogues were designed, synthesized and their biological activities on mushroom tyrosinase were evaluated. Notably, most of compounds displayed remarkable tyrosinase inhibitory activities with IC50 value of lower than 1.0 mu M. Furthermore, the structure-activity relationships (SARs) were discussed and the inhibition mechanism and the inhibitory kinetics of selected compounds 7k and 8d were also investigated. Taken together, these results suggested that such compounds could serve as the promising candidates for the treatment of tyrosinase-related disorders and further development of such compounds might be of great interest. (C) 2015 Published by Elsevier Ltd. |
| WOS关键词 | MUSHROOM TYROSINASE ; BIOLOGICAL EVALUATION ; CINNAMIC ACID ; DERIVATIVES ; MECHANISM ; PHENYLMETHYLENETHIOSEMICARBAZONES ; THIOSEMICARBAZONES ; ANTITYROSINASE ; MELANOGENESIS ; STILBENES |
| 资助项目 | Science and Technology Project of Guangdong Province, China[2009B060700048] ; Shanghai Municipal Natural Science Foundation, China[15ZR1447800] ; Fundamental Research Funds for the Central Universities[00000000] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000349966700002 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276626]  |
| 专题 | 药物靶标结构与功能中心 |
| 通讯作者 | Song, Huacan |
| 作者单位 | 1.Sun Yat Sen Univ, Sch Chem & Chem Engn, Guangzhou 510275, Guangdong, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Struct & Funct Drug Targets, VARI SIMM Ctr,CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | You, Ao,Zhou, Jie,Song, Senchuan,et al. Rational design, synthesis and structure-activity relationships of 4-alkoxy- and 4-acyloxy-phenylethylenethiosemicarbazone analogues as novel tyrosinase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2015,23(5):924-931. |
| APA | You, Ao,Zhou, Jie,Song, Senchuan,Zhu, Guoxun,Song, Huacan,&Yi, Wei.(2015).Rational design, synthesis and structure-activity relationships of 4-alkoxy- and 4-acyloxy-phenylethylenethiosemicarbazone analogues as novel tyrosinase inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,23(5),924-931. |
| MLA | You, Ao,et al."Rational design, synthesis and structure-activity relationships of 4-alkoxy- and 4-acyloxy-phenylethylenethiosemicarbazone analogues as novel tyrosinase inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 23.5(2015):924-931. |
入库方式： OAI收割
来源：上海药物研究所
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