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Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO-1) Inhibitors Based on Ortho-Naphthaquinone-Containing Natural Product

文献类型：期刊论文

作者Zhao, Hongchuan4; Sun, Pu1,2; Guo, Wei1,2; Wang, Yi1; Zhang, Ao2,3,4; Meng, Linghua1,2; Ding, Chunyong2,4
刊名MOLECULES
出版日期2019-03-02
卷号24期号:6页码:11
关键词indoleamine 2 3-dioxygenase 1 immunosuppressive natural product ortho-naphthaquinone molecular docking
ISSN号1420-3049
DOI10.3390/molecules24061059
通讯作者Meng, Linghua(lhmeng@simm.ac.cn) ; Ding, Chunyong(chding@simm.ac.cn)
英文摘要There is great interest in developing small molecules agents capable of reversing tumor immune escape to restore the body's immune system. As an immunosuppressive enzyme, indoleamine 2,3-dioxygenase 1 (IDO-1) is considered a promising target for oncology immunotherapy. Currently, none of IDO-1 inhibitors have been launched for clinical practice yet. Thus, the discovery of new IDO-1 inhibitors is still in great demand. Herein, a series of diverse ortho-naphthaquinone containing natural product derivatives were synthesized as novel IDO-1 inhibitors. Among them, 1-ene-3-ketone-17-hydroxyl derivative 12 exhibited significantly improved enzymatic and cellular inhibitory activity against IDO-1 when compared to initial lead compounds. Besides, the molecular docking study disclosed that the two most potent compounds 11 and 12 have more interactions within the binding pocket of IDO-1 via hydrogen-bonding, which may account for their higher IDO-1 inhibitory activity.
WOS关键词DENDRITIC CELLS ; TANSHINONE I ; CONSTITUENTS ; DERIVATIVES ; SUPPRESSION ; CHEMISTRY
资助项目National Natural Science Foundation of China[21877120] ; National Natural Science Foundation of China[81430080] ; National Program on Key Basic Research Project of China[2015CB910603] ; National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China[2018ZX09711002-010-001] ; Personalized Medicines-Molecular Signature-based Drug Discovery and Development, Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12020320]
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
语种英语
WOS记录号WOS:000465503800035
出版者MDPI
源URL[http://119.78.100.183/handle/2S10ELR8/290050]  
专题新药研究国家重点实验室
通讯作者Meng, Linghua; Ding, Chunyong
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China
2.Univ Chinese Acad Sci, Sch Pharm, Beijing 100049, Peoples R China
3.ShanghaiTech Univ, Sch Life Scienece & Technol, Shanghai 20120, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Zhao, Hongchuan,Sun, Pu,Guo, Wei,et al. Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO-1) Inhibitors Based on Ortho-Naphthaquinone-Containing Natural Product[J]. MOLECULES,2019,24(6):11.
APA Zhao, Hongchuan.,Sun, Pu.,Guo, Wei.,Wang, Yi.,Zhang, Ao.,...&Ding, Chunyong.(2019).Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO-1) Inhibitors Based on Ortho-Naphthaquinone-Containing Natural Product.MOLECULES,24(6),11.
MLA Zhao, Hongchuan,et al."Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO-1) Inhibitors Based on Ortho-Naphthaquinone-Containing Natural Product".MOLECULES 24.6(2019):11.

入库方式： OAI收割

来源：上海药物研究所

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