Exploration of novel piperazine or piperidine constructed non-covalent peptidyl derivatives as proteasome inhibitors

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• 作者：Rangxiao Zhuang^a ; ¹ ; Lixin Gao^b ; ¹ ; Xiaoqing Lv^c ; Jianjun Xi^a ; Li Sheng^b ; Yanmei Zhao^a ; Ruoyu He^a ; Xiaobei Hu^b ; Yidan Shao^a ; Xuwang Pan^a ; Shourong Liu^a ; Weiwei Huang^a ; Yubo Zhou^b ; ^{ybzhou@simm.ac.cn} ; Jia Li^b ; ^{jli@simm.ac.cn} ; Jiankang Zhang^a ; ^{zjk0125@yeah.net}
• 关键词：Proteasome inhibitors ; Piperazine or piperidine ; Non-covalent ; Peptidyl derivatives ; Anti-cancer
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：1056-1070
• 全文大小：1783 K
• 卷排序：126

文摘

Our study focused on the development of non-covalent proteasome inhibitors. Most target compounds were more potent than the approved drug carfilzomib. All the tested compounds exhibited potent anti-proliferative activities. Compound 35 displayed potent ex vivo and in vivo proteasome inhibitory activities. The t1/2 of compound 35 was 2-fold longer than the analogue without piperidine ring.