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Paper | Regular issue | Vol 102, No. 8, 2021, pp.1536-1551
Published online, 8th June, 2021
DOI: 10.3987/COM-21-14481
Synthesis, Characterization, and DRAK2 Inhibitory Activities of Hydroxyaurone Derivatives

Mingsheng Zhao, Chengqiu Dai, Yi Li, Yinan Liu, Jing-Ya Li,* and Xueling Hou*

*State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China


We reported the synthesis of 25 derivatives of hydroxyaurone, which were characterized by 1H NMR, 13C 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 5μM. Most of the synthetic hydroxyaurones exhibited moderate to good inhibitory activities. The IC50 value ranged from 0.81 to 2.42 μM 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 μM. 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.