Identification of Novel β-Lactam Derivatives as Proteasome Inhibitors for Antitumor Therapy
文献类型：期刊论文
| 作者 | Cao, Yu7; Xu, Gaoya1; Gao, Lixin1; Sun, Jingjing7; Zhang, Lu7; Tong, Qiao7; Kong, Limin2; Zhang, Jiankang3; Zhou, Yubo1,4; Liao, Li5 |
| 刊名 | ARCHIV DER PHARMAZIE
 |
| 出版日期 | 2025-11-01 |
| 卷号 | 358期号:11页码:17 |
| 关键词 | antitumor proteasome inhibitors structure-activity relationships beta-lactam |
| ISSN号 | 0365-6233 |
| DOI | 10.1002/ardp.70136 |
| 通讯作者 | Liao, Li(liaoli0101@sina.com) ; Fu, Liping(fuliping100@163.com) ; Xi, Jianjun(xjianjun@foxmail.com) |
| 英文摘要 | A series of dipeptidic proteasome inhibitors with beta-lactam as the C-terminus was designed and synthesized. Biochemical evaluations of their effects on chymotrypsin-like (CT-L) activity revealed that some of them had inhibitory activity against the proteasome, with IC50 values in the micromolar range. Based on the enzymatic results, structure-activity relationships (SAR) were discussed in detail. Some potent compounds were further selected for antiproliferative assays toward multiple cancer cell lines, with compounds 66 and 78 demonstrating activity against RS4;11 cells and IC50 values of less than 1 mu M. Additionally, cellular mechanistic studies indicated that these effects were linked to their ability to inhibit proteasome signal pathways and to induce apoptosis in RS4;11 cells, as demonstrated by flow cytometry. Collectively, these results illustrate that compound 66 is a potent proteasome inhibitor with significant potential as an antitumor agent. |
| WOS关键词 | BORTEZOMIB |
| 资助项目 | This study was funded by the Construction Fund of Key Medical Disciplines of Hangzhou (2025HZZD13), the Zhejiang Provincial Natural Science Foundation of China (LTGY24B020001), the Medical Health Science and Technology Project of Zhejiang Provincial Health |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001629584000014 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/322333]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Liao, Li; Fu, Liping; Xi, Jianjun |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Chem Biol, Shanghai, Peoples R China 2.Zhejiang Univ, Affiliated Hosp 1, Sch Med, Dept Clin Pharm, Hangzhou, Peoples R China 3.Hangzhou City Univ, Sch Med, Key Lab Novel Targets & Drug Study Neural Repair Z, Hangzhou, Peoples R China 4.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, Zhongshan, Peoples R China 5.Hangzhou Childrens Hosp, Dept Pharm, Hangzhou, Peoples R China 6.Zhejiang Chinese Med Univ, Shaoxing TCM Hosp, Dept Pharm, Shaoxing, Peoples R China 7.Hangzhou Xixi Hosp, Dept Pharmaceut Preparat, Hangzhou, Peoples R China |
| 推荐引用方式 GB/T 7714 | Cao, Yu,Xu, Gaoya,Gao, Lixin,et al. Identification of Novel β-Lactam Derivatives as Proteasome Inhibitors for Antitumor Therapy[J]. ARCHIV DER PHARMAZIE,2025,358(11):17. |
| APA | Cao, Yu.,Xu, Gaoya.,Gao, Lixin.,Sun, Jingjing.,Zhang, Lu.,...&Xi, Jianjun.(2025).Identification of Novel β-Lactam Derivatives as Proteasome Inhibitors for Antitumor Therapy.ARCHIV DER PHARMAZIE,358(11),17. |
| MLA | Cao, Yu,et al."Identification of Novel β-Lactam Derivatives as Proteasome Inhibitors for Antitumor Therapy".ARCHIV DER PHARMAZIE 358.11(2025):17. |
入库方式： OAI收割
来源：上海药物研究所
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