Title of article :
Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors
Author/Authors :
Robert M. Borzilleri، نويسنده , , Zhen-wei Cai، نويسنده , , Christopher Ellis، نويسنده , , Joseph Fargnoli، نويسنده , , Aberra Fura، نويسنده , , Tracy Gerhardt، نويسنده , , Bindu Goyal، نويسنده , , John T. Hunt، نويسنده , , Steven Mortillo، نويسنده , , Ligang Qian، نويسنده , , John Tokarski، نويسنده , , Viral Vyas، نويسنده , , Barri Wautlet، نويسنده , , Xioping Zheng، نويسنده , , Rajeev S. Bhide، نويسنده ,
Abstract :
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.
Keywords :
VEGFR-2 , angiogenesis , SAR , Kinase receptor
