4293-71-4Relevant academic research and scientific papers
Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity
Cao, Qi,Han, Xiao,Hou, Yunlei,Liu, Chunyang,Liu, Lei,Meng, Yangyang,Qin, Mingze,Tian, Ye,Wang, Xiaobo,Wu, Xia,Zhang, Haotian,Zheng, Shuaishuai
, (2020)
Structural modifications of compound 2, an angiokinase inhibitor reported by our group were performed, which led to the discovery of methyl (Z)-3-(((4-(2-methyl-5-((4-methylpiperazin-1-yl)methyl)-1H-pyrrol-1-yl)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate (7h). Compound 7h exhibited excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. At the cellular level, compound 7h significantly attenuated phosphorylation of AKT and ERK proteins, potently inhibited colony formation of HT-29, MKN74, and HepG2 cancer cells, and induced cell apoptosis. Upon incubation with human liver microsome, 7h exhibited comparable metabolic stability to nintedanib. Compound 7h has emerged as a promising lead compound for future drug design.
Substituted indolinone derivative and application thereof
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Paragraph 0184; 0186; 0187; 0188, (2017/08/02)
The invention relates to a substituted indolinone derivative represented as the general formula (I) and used as a tyrosine kinase inhibitor, and medicinal acceptable salts or isomers thereof, wherein the R1, R2, R3, R4, R5, R6, R7, n and the ring A are defined as the specifications. The invention also relates to a preparation method of the compound, and an application of the compound in preparation of medicines for prevention or therapy of fibrosis diseases and excess hyperplasia diseases.
