305371-33-9Relevant articles and documents
Identification of a novel class of selective Tpl2 kinase inhibitors: 4-Alkylamino-[1,7]naphthyridine-3-carbonitriles
Kaila, Neelu,Green, Neal,Li, Huan-Qiu,Hu, Yonghan,Janz, Kristin,Gavrin, Lori Krim,Thomason, Jennifer,Tam, Steve,Powell, Dennis,Cuozzo, John,Hall, J. Perry,Telliez, Jean-Baptiste,Hsu, Sang,Nickerson-Nutter, Cheryl,Wang, Qin,Lin, Lih-Ling
, p. 6425 - 6442 (2008/04/05)
We have previously reported the discovery and initial SAR of the [1,7]naphthyridine-3-carbonitriles and quinoline-3-carbonitriles as Tumor Progression Loci-2 (Tpl2) kinase inhibitors. In this paper, we report new SAR efforts which have led to the identifi
Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationships
Gavrin, Lori Krim,Green, Neal,Hu, Yonghan,Janz, Kristin,Kaila, Neelu,Li, Huan-Qiu,Tam, Steve Y.,Thomason, Jennifer R.,Gopalsamy, Ariamala,Ciszewski, Greg,Cuozzo, John W.,Hall, J. Perry,Hsu, Sang,Telliez, Jean-Baptiste,Lin, Lih-Ling
, p. 5288 - 5292 (2007/10/03)
The synthesis and structure-activity studies of a series of 6-substituted-4-anilino-[1,7]-naphthyridine-3-carbonitriles as inhibitors of Tpl2 kinase are described. The early exploratory work described here may lead to the discovery of compounds with signi
Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles
Wissner, Allan,Hamann, Philip R.,Nilakantan, Ramaswamy,Greenberger, Lee M.,Ye, Fei,Rapuano, Timothy A.,Loganzo, Frank
, p. 1411 - 1416 (2007/10/03)
The syntheses and EGFR kinase inhibitory activity of a series of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles are described. Both reversible and irreversible binding inhibitors were prepared. These series were compared with each other and with the corresponding 4-anilinoquinoline-3-carbonitriles. Compounds having a 1,7-naphthyridine core structure can retain high potency while those with a 1,8-naphthyridine core are significantly less active. These results are consistent with molecular modeling observations.