329940-36-5Relevant academic research and scientific papers
The discovery of N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4- oxoquinazolin-3(4H)-yl]benzamide (AZD6703), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases
Brown, Dearg S.,Cumming, John G.,Bethel, Paul,Finlayson, Jonathan,Gerhardt, Stefan,Nash, Ian,Pauptit, Richard A.,Pike, Kurt G.,Reid, Alan,Snelson, Wendy,Swallow, Steve,Thompson, Caroline
scheme or table, p. 3879 - 3883 (2012/07/03)
A novel, potent and selective quinazolinone series of inhibitors of p38α MAP kinase has been identified. Modifications designed to address the issues of poor aqueous solubility and high plasma protein binding as well as embedded aniline functionalities resulted in the identification of a clinical candidate N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin- 3(4H)-yl]benzamide (AZD6703). Optimisation was guided by understanding of the binding modes from X-ray crystallographic studies which showed a switch from DFG 'out' to DFG 'in' as the inhibitor size was reduced to improve overall properties.
Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38α mitogen-activated protein kinase inhibitors
Hynes Jr., John,Dyckman, Alaric J.,Lin, Shuqun,Wrobleski, Stephen T.,Wu, Hong,Gillooly, Kathleen M.,Kanner, Steven B.,Lonial, Herinder,Loo, Derek,McIntyre, Kim W.,Pitt, Sidney,Ding, Ren Shen,Shuster, David J.,Yang, XiaoXia,Zhang, Rosemary,Behnia, Kamelia,Zhang, Hongjian,Marathe, Punit H.,Doweyko, Arthur M.,Tokarski, John S.,Sack, John S.,Pokross, Matthew,Kiefer, Susan E.,Newitt, John A.,Barrish, Joel C.,Dodd, John,Schieven, Gary L.,Leftheris, Katerina
, p. 4 - 16 (2008/09/18)
A novel structural class of p38 mitogen-activated protein (MAP) kinase inhibitors consisting of substituted 4-(phenylamino)-pyrrolo[2,1-f][1,2,4] triazines has been discovered. An initial subdeck screen revealed that the oxindole-pyrrolo[2,1-f][1,2,4]tria
