Medicinal Chemistry

Design, Synthesis and Biological Evaluation of Novel Non-Peptide Boronic Acid Derivatives as Proteasome Inhibitors

J Zhang, L Shen, J Wang, P Luo, Y Hu

文献索引：Zhang, Jiankang; Shen, Luqing; Wang, Jincheng; Luo, Peihua; Hu, Yongzhou Medicinal Chemistry, 2014 , vol. 10, # 1 p. 38 - 45

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被引用次数: 1

摘要

A series of novel non-peptide boronic acid derivatives were designed and synthesized via rational drug design principles. All target compounds were screened for the proteasome inhibitory activities in vitro. Selected compounds (6a and 7j) were evaluated for their cytotoxic activities in vitro. Among these tested compounds, two (6a, 7j) displayed better proteasome inhibitory activities than that of the lead compound PI-083, and compound 6a ...