855863-57-9Relevant academic research and scientific papers
Synthesis and bioevaluation and doking study of 1H-pyrrolo[2,3-b]pyridine derivatives bearing aromatic hydrazone moiety as c-Met inhibitors
Wang, Wenhui,Xu, Shan,Duan, Yongli,Liu, Xiaobo,Li, Xiaojing,Wang, Caolin,Zhao, Bingbing,Zheng, Pengwu,Zhu, Wufu
, p. 315 - 327 (2018)
Two series of aromatic hydrazone derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety (7a–r, 8a–i, 12a–b, 13a–c, 16a–d and 17a–e) were designed, synthesized and evaluated for the IC50 values against four cancer cell lines (A549, HepG2, MCF-7and PC-3). Two selected compounds (7c and 17e) were further evaluated for the activity against c-Met, Flt-3, VEGFR-2 and EGFR kinases. The data indicated that targets compounds were selective for c-Met kinase. And the most promising compound 7c was further studied in terms of dose-dependent, time-dependent and cell apoptosis. Most of the compounds showed excellent cytotoxicity activity, especially the most promising compound 7c with the IC50 values of 0.82 ± 0.08 μM, 1.00 ± 0.11 μM, 0.93 ± 0.28 μM and 0.92 ± 0.17 μM against A549, HepG2, MCF-7 and PC-3 cell lines and 0.506 μM against c-Met kinase. Structure–activity relationships (SARs) and docking studies indicated that the activities of the phenyl hydrazone derivatives (7a–r and 8a–i) were superior to that of the heterocyclic hydrazone series (12a–b, 13a–c, 16a–d and 17a–e). What's more, the further studies indicated that the target compounds can induce apoptosis of A549 cells and arrest efficiently the cell cycle progression in G2/M phase of A549 cells.
PYRROLOPYRIDINE-SUBSTITUTED BENZOL DERIVATIVES FOR TREATING CARDIOVASCULAR DISEASES
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Page/Page column 41-42, (2010/02/12)
The invention relates to benzols containing heteroaryl substitutes of formula (1), a method for the production and the use thereof for producing drugs for treating and/or preventing human and animal diseases, en particular cardiovascular diseases.
