Literature DB >> 15713401

Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.

Robert M Borzilleri1, Zhen-Wei Cai, Christopher Ellis, Joseph Fargnoli, Aberra Fura, Tracy Gerhardt, Bindu Goyal, John T Hunt, Steven Mortillo, Ligang Qian, John Tokarski, Viral Vyas, Barri Wautlet, Xioping Zheng, Rajeev S Bhide.   

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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Year:  2005        PMID: 15713401     DOI: 10.1016/j.bmcl.2004.12.079

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

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  7 in total

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