Chinese Journal of Organic Chemistry >
Design and Synthesis of Alkyl Phenols Inhibitors of Death Associated Apoptotic Protein Kinase 2 (DRAK2)
Received date: 2021-03-29
Revised date: 2021-04-29
Online published: 2021-05-14
Death associated apoptotic protein kinase 2 (DRAK2) is a threonine/serine kinase and a member of the death- associated protein kinase (DAPK) family. Under the action of external stimuli, its overexpression has the ability to induce apoptosis. High glucose, high fat, and certain cellular inflammatory factors can induce the high expression of DRAK2, thereby causing pancreatic β-cell apoptosis. DRAK2 may play a mediating role in the process. Therefore, small molecule inhibitors targeting DRAK2 own good development prospects to treat diabetes. In this work, more than 20 active compounds were obtained through structural modification of the alkylphenols compound 8a, and the structure-activity relationship between them was preliminarily determined.
Zheng Zhang , Chengqiu Dai , Honghong Wu , Jingya Li , Fajun Nan . Design and Synthesis of Alkyl Phenols Inhibitors of Death Associated Apoptotic Protein Kinase 2 (DRAK2)[J]. Chinese Journal of Organic Chemistry, 2021 , 41(8) : 3204 -3213 . DOI: 10.6023/cjoc202103056
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