910818-29-0Relevant articles and documents
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor
Ruel, Rejean,Thibeault, Carl,L'Heureux, Alexandre,Martel, Alain,Cai, Zhen-Wei,Wei, Donna,Qian, Ligang,Barrish, Joel C.,Mathur, Arvind,D'Arienzo, Celia,Hunt, John T.,Kamath, Amrita,Marathe, Punit,Zhang, Yueping,Derbin, George,Wautlet, Barri,Mortillo, Steven,Jeyaseelan Sr., Robert,Henley, Benjamin,Tejwani, Ravindra,Bhide, Rajeev S.,Trainor, George L.,Fargnoli, Joseph,Lombardo, Louis J.
, p. 2985 - 2989 (2008)
We report herein a series of substituted N-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amines as inhibitors of vascular endothelial growth factor receptor-2 tyrosine kinase. Through structure-activity relationship studies, biochemical potency, pharmacokinetics, and kinase selectivity were optimized to afford BMS-645737 (13), a compound with good preclinical in vivo activity against human tumor xenograft models.