918642-60-1Relevant articles and documents
Synthesis and anti-tumor activity of [1,4] dioxino [2,3-f] quinazoline derivatives as dual inhibitors of c-Met and VEGFR-2
Wei, Dengshuai,Fan, Haoru,Zheng, Kun,Qin, Xuemei,Yang, Leifu,Yang, Yajuan,Duan, Ye,Zhang, Qiang,Zeng, Chengchu,Hu, Liming
, (2019/04/27)
Both c-Met and VEGFR-2 were important targets for cancer therapies. In order to develop reversible and non-covalent c-Met and VEGFR-2 dual inhibitors, a series of [1,4]dioxino[2,3-f]quinazoline derivatives were designed and synthesized. The enzyme assay demonstrated that most target compounds had inhibition potency on both c-Met and VEGFR-2 with IC50 values in nanomolar range especially compounds 7m and 7k. Based on further cell proliferation assay in vitro, compound 7k showed significantly anti-tumor activity in vivo on a hepatocellular carcinoma (MHCC97H cells) xenograft mouse model. We docked the compound 7m with c-Met and VEGFR-2 kinases, and interpreted the SAR of these analogues. All results indicated that the target compounds were dual inhibitors of c-Met and VEGFR-2 kinases that held promising potential in cancer therapy.
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors
Zhao, Yanmei,Zhang, Jiankang,Zhuang, Rangxiao,He, Ruoyu,Xi, Jianjun,Pan, Xuwang,Shao, Yidan,Pan, Jinming,Sun, Jingjing,Cai, Zhaobin,Liu, Shourong,Huang, Weiwei,Lv, Xiaoqing
, p. 3195 - 3205 (2017/05/25)
In this study, a series of novel pyridine and pyrimidine-containing derivatives were designed, synthesized and biologically evaluated for their c-Met inhibitory activities. In the biological evaluation, half of the target compounds exhibited moderate to p
Discovery of anilinopyrimidines as dual inhibitors of c-Met and VEGFR-2: Synthesis, SAR, and cellular activity
Zhan, Zhengsheng,Ai, Jing,Liu, Qiufeng,Ji, Yinchun,Chen, Tiantian,Xu, Yechun,Geng, Meiyu,Duan, Wenhu
supporting information, p. 673 - 678 (2014/07/07)
Both c-Met and VEGFR-2 are important targets for cancer therapies. Here we report a series of potent dual c-Met and VEGFR-2 inhibitors bearing an anilinopyrimidine scaffold. Two novel synthetic protocols were employed for rapid analoguing of the designed
