Objective To synthesize a novel chalcone-1,3,4-thiadiazole hybrid and investigate its anticancer effects against NCI-H460 cells. Methods (E)-3-(4-bromophenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one, 1,3-dibromopropane and 1,3,4-thiadiazole-2-thiol were used as chemical materials to synthesize compound ZW97. The NCI-H460 lung cancer cell line was selected to explore the antitumor effects of compound ZW97 in vitro and in vivo. Results Compound ZW97 selectively inhibited cell proliferation against lung cancer cell lines NCI-H460, HCC-44 and NCI-H3122 with IC50 values of 0.15 mu M, 2.06 mu M and 1.17 mu M, respectively. ZW97 suppressed migration and the epithelial-mesenchymal transition process in NCI-H460 cells in a concentration-dependent manner. Based on the kinase activity results and docking analysis, compound ZW97 is a novel tyrosine-protein kinase Met (c-Met kinase) inhibitor. It also inhibited NCI-H460 cell growth in xenograft models without obvious toxicity to normal tissues. Conclusions Compound ZW97 is a potential c-Met inhibitor that might be a promising agent to treat lung cancer by inhibiting the epithelial-mesenchymal transition process.
基金：
Chest Disease Diagnosis and Treatment Special Funding [YXMZK008]
语种：
外文
被引次数：
WOS：
PubmedID：
中科院(CAS)分区：
出版当年[2021]版：
大类|4 区医学
小类|4 区医学：研究与实验4 区药学
最新[2025]版：
大类|4 区医学
小类|4 区医学：研究与实验4 区药学
JCR分区：
出版当年[2020]版：
Q4PHARMACOLOGY & PHARMACYQ4MEDICINE, RESEARCH & EXPERIMENTAL
最新[2023]版：
Q4MEDICINE, RESEARCH & EXPERIMENTALQ4PHARMACOLOGY & PHARMACY
第一作者机构：[1]Shanghai Jiao Tong Univ, Tongren Hosp, Sch Med, Dept Thorac Surg, 1111 Xianxia Rd, Shanghai 200336, Peoples R China[*1]Department of Thoracic Surgery, Tongren Hospital, Shanghai Jiao Tong University, School of Medicine, 1111 Xianxia Road, Changning District, Shanghai, 200336, China
通讯作者：
通讯机构：[1]Shanghai Jiao Tong Univ, Tongren Hosp, Sch Med, Dept Thorac Surg, 1111 Xianxia Rd, Shanghai 200336, Peoples R China[*1]Department of Thoracic Surgery, Tongren Hospital, Shanghai Jiao Tong University, School of Medicine, 1111 Xianxia Road, Changning District, Shanghai, 200336, China
推荐引用方式(GB/T 7714)：
Zhao Wen,Xu Ye,Guo Qingkui,et al.A novel anti-lung cancer agent inhibits proliferation and epithelial-mesenchymal transition[J].JOURNAL OF INTERNATIONAL MEDICAL RESEARCH.2022,50(4):doi:10.1177/03000605211066300.
APA：
Zhao, Wen,Xu, Ye,Guo, Qingkui,Qian, Wenliang,Zhu, Chen&Zheng, Min.(2022).A novel anti-lung cancer agent inhibits proliferation and epithelial-mesenchymal transition.JOURNAL OF INTERNATIONAL MEDICAL RESEARCH,50,(4)
MLA：
Zhao, Wen,et al."A novel anti-lung cancer agent inhibits proliferation and epithelial-mesenchymal transition".JOURNAL OF INTERNATIONAL MEDICAL RESEARCH 50..4(2022)
