Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors |
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| Authors: | Borzilleri Robert M Cai Zhen-Wei Ellis Christopher Fargnoli Joseph Fura Aberra Gerhardt Tracy Goyal Bindu Hunt John T Mortillo Steven Qian Ligang Tokarski John Vyas Viral Wautlet Barri Zheng Xioping Bhide Rajeev S |
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| Affiliation: | Department of Oncology Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. |
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| 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. |
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