945381-57-7Relevant academic research and scientific papers
Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: Synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives
Tang, Peng Cho,Su, Yi Dong,Feng, Jun,Fu, Jian Hong,Yang, Jiang Liang,Xiao, Lu,Peng, Jiang Hua,Li, Ya Li,Zhang, Lei,Hu, Bing,Zhou, Ying,Li, Fang Qiong,Fu, Bei Bei,Lou, Li Guang,Gong, Ai Shen,She, Gao Hong,Sun, Wei Hong,Mong, Xian Tai
, p. 8140 - 8149 (2011/02/23)
The inhibition of receptor tyrosine kinases (RTKs) has become a successful approach in the development of anticancer agents. Many potent small-molecule kinase inhibitors have been discovered. We report herein a series of pyrrolo-fused-heterocycle-2-indolinone analogues as inhibitors of vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), and c-Kit. Among them, some pyrrolo-fused six- and seven-membered-heterocycle derivatives such as 9, 15, 23, and 25 are potent inhibitors of VEGFR, PDGFR, and c-Kit both enzymatically (50 nM) and cellularly (50 nM). Furthermore, compounds 9 and 25 possess favorable pharmacokinetic profiles and demonstrate good efficacies against human HT-29 cell colon tumor xenografts in nude mice. Further evaluations are in progress.
Pyrrolo [3,2-C] Pyridine-4-One 2-Indolinone Protein Kinase Inhibitors
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Page/Page column 55, (2010/02/16)
The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8X, Y and have the meaning cited in the specification.
PYRROLO [3,2-C] PYRIDINE-4-ONE 2-INDOLINONE PROTEIN KINASE INHIBITORS
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Page/Page column 72-73, (2010/11/28)
The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8 X , Y and …. have the meaning cited in the specifica
