503149-31-3Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel non-covalent piperidine-containing peptidyl proteasome inhibitors
Zhang, Jiankang,Gao, Lixin,Xi, Jianjun,Sheng, Li,Zhao, Yanmei,Xu, Lei,Shao, Yidan,Liu, Shourong,Zhuang, Rangxiao,Zhou, Yubo,Li, Jia
, p. 6206 - 6214 (2016)
A series of novel non-covalent piperidine-containing dipeptidyl derivatives were designed, synthesized and evaluated as proteasome inhibitors. All target compounds were tested for their proteasome chymotrypsin-like inhibitory activities, and selected deri
Optimization of piperidine constructed peptidyl derivatives as proteasome inhibitors
Zhao, Yanmei,Xu, Lei,Zhang, Jiankang,Zhang, Mengmeng,Lu, Jingyi,He, Ruoyu,Xi, Jianjun,Zhuang, Rangxiao,Li, Jia,Zhou, Yubo
, (2020/11/27)
A series of non-covalent piperidine-containing peptidyl derivatives with various substituents at side chains of different residues were designed, synthesized and evaluated as proteasome inhibitors. After proteasome inhibitory evaluations of all the synthe
Covalent docking modelling-based discovery of tripeptidyl epoxyketone proteasome inhibitors composed of aliphatic-heterocycles
Dong, Xiao-Wu,Zhang, Jian-Kang,Xu, Lei,Che, Jin-Xin,Cheng, Gang,Hu, Xiao-Bei,Sheng, Li,Gao, An-Hui,Li, Jia,Liu, Tao,Hu, Yong-Zhou,Zhou, Yu-Bo
supporting information, p. 602 - 614 (2019/01/11)
The potential of specific proteasome inhibitors to act as anti-cancer agents has attracted intensive investigations. The proteasome can be covalently inhibited by epoxyketone derivatives via a two-step reaction. Several computational approaches have been developed to mimic the covalent binding event. Compound 1 composed of a six-membered heterocyclic ring was designed by using covalent docking. With a possible different binding mode from the clinical compound Carfilzomib, it occupied the S5 pocket of 20S proteasome and showed favorable inhibitory activity. Subsequently optimization and evaluation were taken place. Among these compounds, 11h demonstrated extraordinary in vitro inhibitory activity and selectivity, and good in vivo proteasome inhibitory activity, a favorable pharmacokinetic profile and xenograft tumor inhibition. The possible binding pattern of compound 11h against proteasome was further fully explored via calculations, providing a theoretical basis for finding potent proteasome inhibitors.
TRIPEPTIDE EPOXYKETONE COMPOUND CONSTRUCTED BY HETEROCYCLE AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0068; 0070, (2017/02/24)
Disclosed are a tripeptide epoxyketone compound, a preparation method thereof, and a use thereof in the preparation of anti-tumor drugs.
Exploration of novel piperazine or piperidine constructed non-covalent peptidyl derivatives as proteasome inhibitors
Zhuang, Rangxiao,Gao, Lixin,Lv, Xiaoqing,Xi, Jianjun,Sheng, Li,Zhao, Yanmei,He, Ruoyu,Hu, Xiaobei,Shao, Yidan,Pan, Xuwang,Liu, Shourong,Huang, Weiwei,Zhou, Yubo,Li, Jia,Zhang, Jiankang
, p. 1056 - 1070 (2017/01/22)
A series of novel piperazine or piperidine-containing non-covalent peptidyl derivatives possessing a neopentyl-asparagine residue were designed, synthesized and evaluated as proteasome inhibitors. All target compounds were screened for their 20S proteasom
THIAZOLIDINE DERIVATIVE AND MEDICINAL USE THEREOF
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Page 45-46, (2010/02/07)
A thiazolidine derivative represented by the formula (I) wherein each symbol is as defined in the specification, and a pharmaceutically acceptable salt thereof exhibit a potent DPP-IV inhibitory activity, and can be provided as an agent for the prophylaxis or treatment of diabetes, an agent for the prophylaxis or treatment of obesity and the like.
