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Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors

文献类型：期刊论文

作者Yu, Jianjun2,5; Liu, Jieyu1,3; Li, Daqiang2; Xu, Lei3,4; Hong, Duidui2; Chang, Shan6; Xu, Lei6; Li, Jia1,3; Liu, Tao2; Zhou, Yubo1,3
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2019-02-15
卷号164页码:423-439
关键词Proteasome inhibitors Macrocyclic dipeptides N-Benzyl amides Metabolic stability
ISSN号0223-5234
DOI10.1016/j.ejmech.2018.12.072
通讯作者Liu, Tao(Lt601@zju.edu.cn) ; Zhou, Yubo(ybzhou@simm.ac.cn)
英文摘要As proteasome inhibitors, a series of novel macrocyclic dipeptide N-benzyl amides were designed, synthesized and evaluated. Most of them exhibited potent proteasome inhibition and excellent anti-proliferative activity against RPMI 8226, MM1S, and MV-4-11 cell lines. As the most distinguished one among this series, compound 23h displayed potent and selective proteasome inhibitory potency (IC50: beta 5c = 29 nM, beta 5i = 35 nM, beta(1c), beta(2c), beta(1i), beta(2i)> 10 mu M), excellent anti-proliferative activity against RPMI 8226, MM1S, and MV-4-11 cell lines with IC50 values of 18 nM, 15 nM, and 21 nM, respectively, as well as favorable metabolic stability in human liver microsomes (HLMs), highlighting that it is a promising lead compound for further development of proteasome inhibitors. (C) 2019 Elsevier Masson SAS. All rights reserved.
WOS关键词CHYMOTRYPSIN-LIKE ACTIVITY ; BIOLOGICAL EVALUATION ; SELECTIVE INHIBITORS ; 20S PROTEASOME ; DERIVATIVES ; IMMUNOPROTEASOME ; DESIGN ; POTENT ; BORTEZOMIB ; DOCKING
资助项目key project of Zhejiang Provincial Natural Science Foundation of China[LZ15H300001] ; Science and Technology Commission of Shanghai Municipality[17431903000]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000458221400030
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/290630]  
专题新药研究国家重点实验室
通讯作者Liu, Tao; Zhou, Yubo
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China
2.Zhejiang Univ, Coll Pharmaceut Sci, Zhejiang Prov Key Lab Anticanc Drug Res, ZJU ENS Joint Lab Med Chem, Hangzhou 310058, Zhejiang, Peoples R China
3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
4.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201203, Peoples R China
5.Jinan Univ, Sch Pharm, 601 Huangpu Ave West, Guangzhou 510632, Guangdong, Peoples R China
6.Jiangsu Univ Technol, Sch Elect & Informat Engn, Inst Bioinformat & Med Engn, Changzhou 213001, Peoples R China
推荐引用方式
GB/T 7714		 Yu, Jianjun,Liu, Jieyu,Li, Daqiang,et al. Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2019,164:423-439.
APA Yu, Jianjun.,Liu, Jieyu.,Li, Daqiang.,Xu, Lei.,Hong, Duidui.,...&Zhou, Yubo.(2019).Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,164,423-439.
MLA Yu, Jianjun,et al."Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 164(2019):423-439.

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来源：上海药物研究所

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