Synthesis and structure–activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors

RR Khanwelkar, GS Chen, HC Wang, CW Yu…

文献索引：Khanwelkar, Rahul R.; Chen, Grace Shiahuy; Wang, Hsiao-Chun; Yu, Chao-Wu; Huang, Chiung-Hua; Lee, On; Chen, Chih-Hung; Hwang, Chrong-Shiong; Ko, Ching-Huai; Chou, Nien-Tzu; Lin, Mai-Wei; Wang, Ling-Mei; Chen, Yen-Chun; Hseu, Tzong-Hsiung; Chang, Chia-Ni; Hsu, Hui-Chun; Lin, Hui-Chi; Shih, Ying-Chu; Chou, Shuen-Hsiang; Tseng, Hsiang-Wen; Liu, Chih-Peng; Tu, Chia-Mu; Hu, Tsan-Lin; Tsai, Yuan-Jang; Chern, Ji-Wang Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 13 p. 4674 - 4686

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被引用次数: 18

摘要

A series of new ureidoindolin-2-one derivatives were synthesized and evaluated as inhibitors of receptor tyrosine kinases. Investigation of structure–activity relationships at positions 5, 6, and 7 of the oxindole skeleton led to the identification of 6-ureido-substituted 3-pyrrolemethylidene-2-oxindole derivatives that potently inhibited both the vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor ( ...