Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine-a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays
We describe the identification of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine (3), a potent, orally active Src inhibitor with desirable PK properties, demonstrated activity in human tumor cell lines
Noronha, Glenn,Barrett, Kathy,Boccia, Antonio,Brodhag, Tessa,Cao, Jianguo,Chow, Chun P.,Dneprovskaia, Elena,Doukas, John,Fine, Richard,Gong, Xianchang,Gritzen, Colleen,Gu, Hong,Hanna, Ehab,Hood, John D.,Hu, Steven,Kang, Xinshan,Key, Jann,Klebansky, Boris,Kousba, Ahmed,Li, Ge,Lohse, Dan,Mak, Chi Ching,McPherson, Andrew,Palanki, Moorthy S.S.,Pathak, Ved P.,Renick, Joel,Shi, Feng,Soll, Richard,Splittgerber, Ute,Stoughton, Silva,Tang, Suhan,Yee, Shiyin,Zeng, Binqi,Zhao, Ningning,Zhu, Hong
p. 602 - 608
(2007/10/03)
Benzotriazine inhibitors of kinases
The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.
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Page/Page column 66-67
(2008/06/13)
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