849217-58-9Relevant articles and documents
Targeted protein degradation c-Met degradation agent as well as preparation method and application thereof
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, (2021/01/29)
The invention discloses a targeted protein degradation c-Met degradation agent as well as a preparation method and application thereof. The invention provides a c-Met degradation agent based on a targeted protein degradation PROTAC strategy, a preparation
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.
Compound with sulfonyl phenylamine pyrimidine structure and application of compound as antitumor medicine
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, (2019/11/13)
The invention discloses a compound with a sulfonyl phenylamine pyrimidine structure and application of the compound as an antitumor medicine. Pharmacology experiments show that the compound has multi-target inhibition activity, has good multi-target inhib