Development of anti-fungal pesticides from protein kinase inhibitor-based anticancer agents
文献类型： 外文期刊
作者： Ma, Yihui 1 ; Liang, Shen 2 ; Zhang, Yongchao 1 ; Yang, Dangwei 1 ; Wang, Ruofei 2 ;
作者机构： 1.Henan Acad Agr Sci, Plant Protect Inst, Zhengzhou 450002, Henan, Peoples R China
2.Henan Acad Agr Sci, Hort Inst, Zhengzhou 450002, Henan, Peoples R China
关键词： Drug-repurposing discovery; Protein kinase inhibitor; Lead optimization; Antifungal agrochemical
期刊名称：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY （ 影响因子：6.514； 五年影响因子：6.099 ）
ISSN： 0223-5234
年卷期： 2018 年 148 卷
页码：
收录情况： SCI
摘要： Repurposing the novel p21-activated protein kinase inhibitor compound 15 identified its antifungal activity against five selected species of phytopathogenic fungi. Lead optimization based on its structure gave rise to a focused library of 20 derivatives, among which compound 3c demonstrated increased activity over compound 15 and even comparable to that of some commercialized fungicides in the market including carbendazim, tebuconazole, and pyraclostrobin. This study showed that p21-activated protein kinase inhibitor compound 15 was able to serve as a molecular platform to develop effective fungicides against fungal phytopathogens and indicate that screening existing protein kinase inhibitors might be an effective way to identify lead compounds for antifungal pesticides development. (C) 2018 Elsevier Masson SAS. All rights reserved.
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