中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
首页 机构 成果 学者
  
  1. CAS IR Grid
  2. 合肥物质科学研究院
  3. 中国科学院合肥物质科学研究院
S3I-201 derivative incorporating naphthoquinone unit as effective STAT3 inhibitors: Design, synthesis and anti-gastric cancer evaluation

文献类型：期刊论文

作者Li, Haobin2; Cai, Maohua2; Cao, Fei4; Yu, Dehua2; Yang, Jing2; Yu, Wenkai2; Chu, Chu4; Guan, Xiaoqing1,3; Qin, Jiang-Jiang1,2,3; Dong, Jinyun1,2,3
刊名BIOORGANIC & MEDICINAL CHEMISTRY
出版日期2022-10-01
卷号71
ISSN号0968-0896
关键词STAT3 inhibitor Quinone derivative S3I-201 Anti -gastric cancer drug
DOI10.1016/j.bmc.2022.116941
通讯作者Qin, Jiang-Jiang(jqin@ucas.ac.cn) ; Dong, Jinyun(dongjy@ibmc.ac.cn)
英文摘要Signal transducer and activator of transcription 3 (STAT3) is a key regulator of many human cancers and has been widely recognized as a promising target for cancer therapy. A variety of small-molecule inhibitors have been developed for targeting STAT3, and some of them are now undergoing clinical trials. S3I-201, a known STAT3 inhibitor, may block STAT3 function in cancer cells by binding to the STAT3 SH2 domain to disrupt STAT3 protein complex formation. Using S3I-201 as a starting point for drug development, we synthesized a series of new STAT3 inhibitors 9a-x in this study by introducing naphthoquinone unit, a privileged fragment in STAT3 inhibitors. Most of the compounds exhibited strong anti-proliferation activity of gastric cancer cells (MGC803, MKN28, MNK1, and AGS). The representative compound 9n (SIL-14) could effectively inhibit the colony formation and migration of gastric cancer cells MGC803, arrest the cell cycle and induce MGC803 cell apoptosis at low micromolar concentrations in vitro. In addition, SIL-14 can also inhibit the phosphorylation of STAT3 protein and significantly decrease the expression of total STAT3, suggesting that it may exert anticancer effects by blocking the STAT3 signaling pathway. These results support that SIL-14 may be a promising STAT3 inhibitor for the further development of potential anti-gastric cancer candidates.
WOS关键词SIGNAL TRANSDUCER ; TRANSCRIPTION ; DISCOVERY ; ACTIVATOR ; ACID
资助项目Zhejiang Provincial Natural Science Foundation of China[LQ21B020003] ; National Natural Science Foundation of China[82103967] ; Key Laboratory of Prevention, Diagnosis and Therapy of Upper Gastrointestinal Cancer of Zhejiang Province[2022E10021] ; Program of Zhejiang Provincial TCM Sci-tech Plan[2020ZZ005]
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种英语
出版者PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号WOS:000860419100002
资助机构Zhejiang Provincial Natural Science Foundation of China ; National Natural Science Foundation of China ; Key Laboratory of Prevention, Diagnosis and Therapy of Upper Gastrointestinal Cancer of Zhejiang Province ; Program of Zhejiang Provincial TCM Sci-tech Plan
源URL[http://ir.hfcas.ac.cn:8080/handle/334002/129173]  
专题中国科学院合肥物质科学研究院
通讯作者Qin, Jiang-Jiang; Dong, Jinyun
作者单位1.Chinese Acad Sci, Inst Basic Med & Canc IBMC, Hangzhou 310018, Zhejiang, Peoples R China
2.Zhejiang Chinese Med Univ, Sch Pharmaceut Sci, Hangzhou 310053, Peoples R China
3.Univ Chinese Acad Sci, Canc Hosp, Zhejiang Canc Hosp, Hangzhou 310022, Zhejiang, Peoples R China
4.Zhejiang Univ Technol, Coll Pharmaceut Sci, Hangzhou 310032, Peoples R China
推荐引用方式
GB/T 7714		 Li, Haobin,Cai, Maohua,Cao, Fei,et al. S3I-201 derivative incorporating naphthoquinone unit as effective STAT3 inhibitors: Design, synthesis and anti-gastric cancer evaluation[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2022,71.
APA Li, Haobin.,Cai, Maohua.,Cao, Fei.,Yu, Dehua.,Yang, Jing.,...&Dong, Jinyun.(2022).S3I-201 derivative incorporating naphthoquinone unit as effective STAT3 inhibitors: Design, synthesis and anti-gastric cancer evaluation.BIOORGANIC & MEDICINAL CHEMISTRY,71.
MLA Li, Haobin,et al."S3I-201 derivative incorporating naphthoquinone unit as effective STAT3 inhibitors: Design, synthesis and anti-gastric cancer evaluation".BIOORGANIC & MEDICINAL CHEMISTRY 71(2022).

入库方式： OAI收割

来源：合肥物质科学研究院

浏览0
下载0
收藏0
其他版本

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。