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ID: ALA1140398

Journal: Bioorg Med Chem Lett

Title: New dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Authors: Fink BE, Vite GD, Mastalerz H, Kadow JF, Kim SH, Leavitt KJ, Du K, Crews D, Mitt T, Wong TW, Hunt JT, Vyas DM, Tokarski JS.

Abstract: A novel series of dual EGFR and HER2 inhibitors based on the pyrrolo[2,1-f][1,2,4]triazine nucleus is described. A general route toward their synthesis, which enables functionalization at multiple sites, has been developed. Biological evaluation in enzymatic and cell-based assays has identified a series of C-6 carbamates with potent biochemical and cellular activities.

CiteXplore: 16111887

DOI: 10.1016/j.bmcl.2005.07.027