Synthesis, activity evaluation, and docking analysis of barbituric acid aryl hydrazone derivatives as RSK2 inhibitors

…, W Lu, J Huang, H Li, Y Xu, X Liu, Z Zhao

文献索引：Xue, Mengzhu; Xu, Minghao; Lu, Weiqiang; Huang, Jin; Li, Honglin; Xu, Yufang; Liu, Xiaofeng; Zhao, Zhenjiang Journal of Enzyme Inhibition and Medicinal Chemistry, 2013 , vol. 28, # 4 p. 747 - 752

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被引用次数: 4

摘要

The 90 kDa ribosomal S6 kinases (RSKs), especially RSK2, have attracted attention for the development of new anticancer agents. Through structural optimization of the hit compound 1 from our previous study, a series of barbituric acid aryl hydrazone analogues were designed and synthesized as potential RSK2 inhibitors. The most potent one, compound 9, showed a higher activity against RSK2 with an IC50 value of 1.95 μM. To analyze and ...