Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.

@article{Sun2003DiscoveryO5,
  title={Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.},
  author={Li Sun and Chris Liang and Sheri Shirazian and Yong Zhou and Todd F. Miller and Jean Cui and Juri Y. Fukuda and Ji-Yu Chu and Asaad S. Nematalla and Xueyan Wang and Hui Chen and Anand Sistla and Tony C. Luu and Flora Tang and James Wei and C. Peng Moraga Tang},
  journal={Journal of medicinal chemistry},
  year={2003},
  volume={46 7},
  pages={
          1116-9
        }
}
To improve the antitumor properties and optimize the pharmaceutical properties including solubility and protein binding of indolin-2-ones, a number of different basic and weakly basic analogues were designed and synthesized. 5-[5-Fluoro-2-oxo-1,2-dihydroindol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide (12b or SU11248) has been found to show the best overall profile in terms of potency for the VEGF-R2 and PDGF-Rbeta tyrosine kinase at biochemical and… CONTINUE READING
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