1345847-73-5Relevant academic research and scientific papers
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.
Efficient and divergent synthesis of functionalized cyclopropanes via iodoform reaction
Zhang, Dingyuan,Zhang, Rui,Xiang, Dexuan,Zhang, Ning,Liang, Yongjiu,Dong, Dewen
experimental part, p. 705 - 710 (2012/04/04)
Efficient and divergent one-pot synthesis of cyclopropyl amides and esters from readily available 1-acetylcyclopropanes via iodoform reaction based on the selection of reaction conditions is reported. A series of substituted cyclopropyl amides were synthe
CYCLOPROPYL DICARBOXAMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITES
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Page/Page column 33, (2011/11/13)
The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: Formula I or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer, or tautomer thereof.
