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SYNTHESIS, CHARACTERIZATION, AND DRAK2 INHIBITORY ACTIVITIES OF HYDROXYAURONEDERIVATIVESURONE DERIVATIVES

文献类型：期刊论文

作者Zhao, Mingsheng2,3; Dai, Chengqiu1,4; Li, Yi2,3; Liu, Yinan1; Li, Jing-Ya1; Hou, Xueling2
刊名HETEROCYCLES
出版日期2021
卷号102期号:8页码:1536-1551
ISSN号0385-5414
DOI10.3987/COM-21-14481
通讯作者Li, Jing-Ya(jyli@simm.ac.cn) ; Hou, Xueling(xlhou@ms.xjb.ac.cn)
英文摘要We reported the synthesis of 25 derivatives of hydroxyaurone, which were characterized by H-1 NMR, C-13 NMR, high resolution mass spectrum, and single crystal X-ray diffraction analysis. Their activities on the death-associated protein kinase-related apoptosis-inducing kinase-2 (DRAK2) were evaluated by kinase detection kit at a dosage of 5 mu M. Most of the synthetic hydroxyaurones exhibited moderate to good inhibitory activities. The IC50 value ranged from 0.81 to 2.42 mu M when the structure of aurone's B ring was kept unchanged and its A ring was substituted by hydroxyl groups. On the contrary, modification of the aurone's B-ring with hydroxyl groups lead to the IC50 value ranging from 1.15 to 17.5 mu M. This indicates presence of hydroxyl group of the B ring is crucial for aurone's DRAK2 kinase inhibitors. Therefore, hydroxyaurone may serve as a new possible lead compound for the discovery of DRAK2. Further pharmacological investigations are underway and will be reported in due course.
WOS关键词MULTIFUNCTIONAL AGENTS ; DISCOVERY ; AURONES ; APOPTOSIS ; KINASE ; CELLS ; OXIDE
资助项目National Key R&D Program of China[2020YFE0205600] ; Central Asian Center of Drug Research and Development, Chinese Academy of Sciences[CAM201904] ; Central Asian Center of Drug Research and Development, Chinese Academy of Sciences[CAM202001] ; One Belt One Road Youth Exchange Program of Shanghai Municipal Committee of Science and Technology[19430742000]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000719567100005
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/298985]  
专题中国科学院上海药物研究所
通讯作者Li, Jing-Ya; Hou, Xueling
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Chinese Natl Ctr Drug Screening, Shanghai 310115, Peoples R China
2.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Urumqi 830011, Peoples R China
3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
4.Chinese Acad Sci, Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Hangzhou 310024, Peoples R China
推荐引用方式
GB/T 7714		 Zhao, Mingsheng,Dai, Chengqiu,Li, Yi,et al. SYNTHESIS, CHARACTERIZATION, AND DRAK2 INHIBITORY ACTIVITIES OF HYDROXYAURONEDERIVATIVESURONE DERIVATIVES[J]. HETEROCYCLES,2021,102(8):1536-1551.
APA Zhao, Mingsheng,Dai, Chengqiu,Li, Yi,Liu, Yinan,Li, Jing-Ya,&Hou, Xueling.(2021).SYNTHESIS, CHARACTERIZATION, AND DRAK2 INHIBITORY ACTIVITIES OF HYDROXYAURONEDERIVATIVESURONE DERIVATIVES.HETEROCYCLES,102(8),1536-1551.
MLA Zhao, Mingsheng,et al."SYNTHESIS, CHARACTERIZATION, AND DRAK2 INHIBITORY ACTIVITIES OF HYDROXYAURONEDERIVATIVESURONE DERIVATIVES".HETEROCYCLES 102.8(2021):1536-1551.

入库方式： OAI收割

来源：上海药物研究所

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