310442-33-2

Upstream product

• 310442-40-1 methyl 4-chloro-5-methylpyrrolo[2,1-f][1,2,4]triazine-6-carboxylate 
• 310431-29-9 5-methyl-4-oxo-3,4-dihydro-pyrrolo[2,1-f][1,2,4]triazine-6-carboxylic acid methyl ester 
• 3780-42-5 dimethyl 3-methyl-1H-pyrrole-2,4-dicarboxylate 
• 40318-15-8 methyl 4-methyl-1H-pyrrole-3-carboxylate 
• 310431-26-6 dimethyl 1-amino-3-methyl-1H-pyrrole-2,4-dicarboxylate 
• 310442-32-1 4-[(3-Hydroxy-4-methylphenyl)amino]-5-methylpyrrolo[2,1-f][1,2,4]triazine-6-carboxylic acid methyl ester 

Relevant academic research and scientific papers

Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors

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.

Pyrrolotriazine inhibitors of kinases

The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.