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Bioactivity-Driven Synthesis of the Marine Natural Product Naamidine J and Its Derivatives as Potential Tumor Immunological Agents by Inhibiting Programmed Death-Ligand 1

文献类型：期刊论文

作者Fu, Pan-Pan2,3; Wang, Qun1; Zhang, Qing1; Jin, Yang3; Liu, Jin3; Chen, Kai-Xian3; Guo, Yue-Wei2,3; Liu, San-Hong1; Li, Xu-Wen2,3
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2023-04-27
卷号66期号:8页码:5427-5438
DOI10.1021/acs.jmedchem.2c01702
文献子类Article
英文摘要The total synthesis of the marine natural product naamidine J and a rapid structure modification toward its derivatives were achieved on the basis of several rounds of structure-relationship analyses of their tumor immunological activities. These compounds were tested for programmed death-ligand 1 (PD-L1) protein expression in human colorectal adenocarcinoma RKO cells. Among them, compound 11c was found to efficiently suppress constitutive PD-L1 expression in RKO cells with low toxicity and further exerted its antitumor effect in MC38 tumor-bearing C57BL/6 mice by reducing PD-L1 expression and enhancing tumor-infiltrating T-cell immunity. This research work may provide insight for the discovery of new marine natural product-derived tumor immunological drug leads.
WOS关键词IMIDAZOLE ALKALOIDS ; CONCISE
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000971983800001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/309647]  
专题新药研究国家重点实验室
通讯作者Guo, Yue-Wei; Liu, San-Hong; Li, Xu-Wen
作者单位1.Shanghai Univ Tradit Chinese Med, Inst Interdisciplinary Integrat Med Res, Shanghai Frontiers Sci Ctr TCM Chem Biol, Shanghai 201203, Peoples R China
2.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China;
3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Fu, Pan-Pan,Wang, Qun,Zhang, Qing,et al. Bioactivity-Driven Synthesis of the Marine Natural Product Naamidine J and Its Derivatives as Potential Tumor Immunological Agents by Inhibiting Programmed Death-Ligand 1[J]. JOURNAL OF MEDICINAL CHEMISTRY,2023,66(8):5427-5438.
APA Fu, Pan-Pan.,Wang, Qun.,Zhang, Qing.,Jin, Yang.,Liu, Jin.,...&Li, Xu-Wen.(2023).Bioactivity-Driven Synthesis of the Marine Natural Product Naamidine J and Its Derivatives as Potential Tumor Immunological Agents by Inhibiting Programmed Death-Ligand 1.JOURNAL OF MEDICINAL CHEMISTRY,66(8),5427-5438.
MLA Fu, Pan-Pan,et al."Bioactivity-Driven Synthesis of the Marine Natural Product Naamidine J and Its Derivatives as Potential Tumor Immunological Agents by Inhibiting Programmed Death-Ligand 1".JOURNAL OF MEDICINAL CHEMISTRY 66.8(2023):5427-5438.

入库方式： OAI收割

来源：上海药物研究所

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