915145-15-2Relevant academic research and scientific papers
Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy) phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): A topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degene
Palanki, Moorthy S. S.,Akiyama, Hideo,Campochiaro, Peter,Cao, Jianguo,Chow, Chun P.,Dellamary, Luis,Doukas, John,Fine, Richard,Gritzen, Colleen,Hood, John D.,Hu, Steven,Kachi, Shu,Kang, Xinshan,Klebansky, Boris,Kousba, Ahmed,Lohse, Dan,Chi, Ching Mak,Martin, Michael,McPherson, Andrew,Pathak, Ved P.,Renick, Joel,Soll, Richard,Umeda, Naoyasu,Yee, Shiyin,Yokoi, Katsutoshi,Zeng, Binqi,Zhu, Hong,Noronha, Glenn
, p. 1546 - 1559 (2008/12/21)
Age-related macular degeneration (AMD) is one of the leading causes of loss of vision in the industrialized world. Attenuating the VEGF signal in the eye to treat AMD has been validated clinically. A large body of evidence suggests that inhibitors targeti
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
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)
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
The design and preliminary structure-activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes
Cao, Jianguo,Fine, Richard,Gritzen, Colleen,Hood, John,Kang, Xinshan,Klebansky, Boris,Lohse, Dan,Mak, Chi Ching,McPherson, Andrew,Noronha, Glenn,Palanki, Moorthy S.S.,Pathak, Ved P.,Renick, Joel,Soll, Richard,Zeng, Binqi,Zhu, Hong
, p. 5812 - 5818 (2008/03/14)
We describe the design, synthesis and structure-activity relationship studies in optimizing a series of benzotriazine compounds as potent inhibitors of both Abl and Abl-T315I enzymes. The design includes targeting of an acid functional residue on the αC-h
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors
Noronha, Glenn,Barrett, Kathy,Cao, Jianguo,Dneprovskaia, Elena,Fine, Richard,Gong, Xianchang,Gritzen, Colleen,Hood, John,Kang, Xinshan,Klebansky, Boris,Li,Liao,Lohse, Dan,Mak, Chi Ching,McPherson, Andrew,Palanki, Moorthy S.S.,Pathak, Ved P.,Renick, Joel,Soll, Richard,Splittgerber, Ute,Wrasidlo, Wolfgang,Zeng, Binqi,Zhao, Ningning,Zhou
, p. 5546 - 5550 (2007/10/03)
We report the discovery and preliminary SAR studies of a series of structurally novel benzotriazine core based small molecules as inhibitors of Src kinase. To the best of our knowledge, benzotriazine template based compounds have not been reported as kina
