310442-33-2Relevant articles and documents
Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors
Borzilleri, Robert M.,Cai, Zhen-Wei,Ellis, Christopher,Fargnoli, Joseph,Fura, Aberra,Gerhardt, Tracy,Goyal, Bindu,Hunt, John T.,Mortillo, Steven,Qian, Ligang,Tokarski, John,Vyas, Viral,Wautlet, Barri,Zheng, Xioping,Bhide, Rajeev S.
, p. 1429 - 1433 (2005)
A versatile synthesis of the suitably functionalized pyrrolo[2,1-f][1,2,4] triazine nucleus is described. SAR at the C-5 and C-6 positions of the 4-(3-hydroxy-4-methylphenylamino)pyrrolo[2,1-f][1,2,4]triazine template led to compounds with good in vitro potency against VEGFR-2 kinase. Glucuronidation of the phenol group is mitigated by incorporation of a basic amino group on the C-6 side chain of the pyrrolotriazine nucleus.