1315588-29-4

Upstream product

• 918538-06-4 2-chloro-N-(5-methyl-1H-pyrazol-3-yl)pyrrolo[2.1-f][1,2,4]triazin-4-amine 
• 79-04-9 chloroacetyl chloride 
• 1193-02-8 4-aminotiophenol 

Downstream Products

• 1315585-15-9 N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)pyrrolo[2,1-f][1,2,4]triazin-2-ylthio)phenyl)-2-(3-hydroxypiperidin-1-yl)acetamide 
• 1315585-20-6 N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)pyrrolo[2,1-f][1,2,4]triazin-2-ylthio)phenyl)-2-((S)-2-(hydroxymethyl)pyrrolidin-1-yl)acetamide 
• 1315585-13-7 N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)pyrrolo[2,1-f][1,2,4]triazin-2-ylthio)phenyl)-2-(dimethylamino)acetamide 
• 1315585-28-4 N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)pyrrolo[2,1-f][1,2,4]triazin-2-ylthio)phenyl)-2-((R)-3-hydroxypyrrolidin-1-yl)acetamide 
• 1315585-21-7 N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)pyrrolo[2,1-f][1,2,4]triazin-2-ylthio)phenyl)-2-((S)-3-hydroxypyrrolidin-1-yl)acetamide 
• 1315585-16-0 N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)pyrrolo[2,1-f][1,2,4]triazin-2-ylthio)phenyl)-2-(N-(2-hydroxyethyl)-N-methylamino)acetamide 
• 1315585-40-0 2-((2S,4S)-2-(hydroxymethyl)-4-methoxypyrrolidin-1-yl)-N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)pyrrolo[2,1-f][1,2,4]triazin-2-ylthio)phenyl)acetamide 
• 1315585-86-4 2-(3-tert-butoxy-4-(hydroxyimino)pyrrolidin-1-yl)-N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)pyrrolo[2,1-f][1,2,4]triazin-2-ylthio)phenyl)acetamide 
• 1315586-37-8 (R)-2-(3-(tert-butylthio)pyrrolidin-1-yl)-N-(4-(4-((5-methyl-1H-pyrazol-3-ylamino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)thio)phenyl)acetamide 
• 1315589-60-6 2-((2S,4R)-4-amino-2-(hydroxymethyl)pyrrolidin-1-yl)-N-(4-((4-((5-methyl-1H-pyrazol-3-yl)amino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)thio)phenyl)acetamide 
• 1315585-75-1 C₂₉H₂₉FN₈O₃S 
• 1315585-26-2 C₂₇H₃₄N₈O₃S 
• 1315590-78-3 2-((2S,4R)-4-hydroxy-2-(hydroxymethyl)pyrrolidin-1-yl)-N-(4-((4-((5-methyl-1H-pyrazol-3-yl)amino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)thio)phenyl)acetamide 
• 1315585-53-5 2-((2S,4S)-4-fluoro-2-(hydroxymethyl)pyrrolidin-1-yl)-N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)pyrrolo[2,1-f][1,2,4]triazin-2-ylthio)phenyl)acetamide 

Relevant academic research and scientific papers

AURORA KINASE COMPOUNDS AND METHODS OF THEIR USE

Provided herein are pyrrolotriazine compounds for treatment of Aurora kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.

Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors

The synthesis and SAR for a novel series of pyrrolotriazines as pan-Aurora kinase inhibitors are described. Optimization of the cyclopropane carboxamide terminus of lead compound 1 resulted in analogs with high cellular activity and improved rat PK profiles. Notably, compound 17l demonstrated tumor growth inhibition in a mouse xenograft model.