Synthesis, in Vitro and in Vivo Biological Evaluation, and Comprehensive Understanding of Structure− Activity Relationships of Dipeptidyl Boronic Acid Proteasome …

…, G Wu, X Zhu, Y Ma, X Zhao, Y Li, Y Yuan…

Index: Zhu, Yongqiang; Wu, Gang; Zhu, Xinrong; Ma, Yuheng; Zhao, Xin; Li, Yuejie; Yuan, Yunxia; Yang, Jie; Yu, Sen; Shao, Feng; Lei, Meng Journal of Medicinal Chemistry, 2010 , vol. 53, # 24 p. 8619 - 8626

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Citation Number: 23

Abstract

An extensive structure− activity relationship (SAR) study of 72 dipeptidyl boronic acid proteasome inhibitors constructed from β-amino acids is reported. SAR analysis revealed that bicyclic groups at the R1 position, 3-F substituents at the R2 position, and bulky aliphatic groups at the R3 position were favorable to the activities. Enzymatic screening results showed that compound 78, comprising all of these features, was the most active inhibitor ...