Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates

S Kawamura, Y Unno, A Asai, M Arisawa…

文献索引：Kawamura, Shuhei; Unno, Yuka; Hirokawa, Takatsugu; Asai, Akira; Arisawa, Mitsuhiro; Shuto, Satoshi Chemical Communications, 2014 , vol. 50, # 19 p. 2445 - 2447

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被引用次数: 6

摘要

We previously developed highly potent proteasome inhibitor 1 (IC50= 5.7 nM) and its nonpeptide derivative 2 (IC50= 29 nM) by systematic structure–activity relationship studies of the peptidic natural product belactosin A and subsequent rational topology-based scaffold hopping, respectively. Their cell growth inhibitory activities, however, were only moderate (IC50= 1.8 μM (1) and> 10 μM (2)). We therefore planned to replace the unstable β- ...