819056-61-6Relevant articles and documents
Aminopyrimido pyrazole/pyrrole derivatives and preparation method and application thereof
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Paragraph 0119; 0124; 0125, (2021/06/21)
The invention relates to aminopyrimidinopyrazole/pyrrole derivatives as well as a preparation method and application thereof, belonging to the field of medicines. The invention provides compounds derivatives as shown in a formula I which is described in the specification and optical isomers thereof, and further provides pharmaceutically acceptable salts of the compounds or the optical isomers thereof. Biological experiments prove that the compounds can remarkably inhibit proliferation of various cancer cells such as breast cancer, lung cancer, colorectal cancer, gastric cancer, bile duct cancer and urothelium carcinoma, have a broad-spectrum anticancer effect, also show an inhibiting effect on proliferation of fibroblasts and hepatic stellate cells, can inhibit growth of tumors in vivo, have wide application prospects and provide a new choice for the development of anti-tumor and anti-fibrosis medicines.
Discovery of novel anti-angiogenesis agents. Part 7: Multitarget inhibitors of VEGFR-2, TIE-2 and EphB4
Li, Chuansheng,Shan, Yuanyuan,Sun, Ying,Si, Ru,Liang, Liyuan,Pan, Xiaoyan,Wang, Binghe,Zhang, Jie
, p. 506 - 518 (2017/11/14)
Herein, we embarked on a structural optimization campaign aiming at the discovery of second generation anti-angiogenesis agents with our previously reported BPS-7 as lead compound. A library of 27 compounds has been afforded based on the highly conserved ATP-binding pocket of VEGFR-2, Tie-2, and EphB4. Several title compounds exhibited simultaneous inhibitory effects against three angiogenic RTKs. These compounds with a ‘triplet’ inhibition profile have been identified as novel anti-angiogenic and anticancer agents. The representative VDAU11 displayed prominent anti-angiogenic and anticancer potency and could be considered as a candidate for further optimization. These results indicate that N-(pyridin-2-yl)acrylamide could serve as a novel hinge-binding group of triple inhibitors.