The kinase activity of epidermal growth factor receptor (EGFR) is the target of a several commercial antineoplastic agents such as Tarceva and Iressa. Despite their efficacy, EGFR kinase inhibitors can be often plagued by moderate antiproliferative activity against certain tumour types in the clinic. To circumvent the traditional pathway and using structure based design techniques, dual action compounds termed 'combi-molecules' were designed and investigated to examine a synergistic approach targeting both EGFR kinase and Src kinase or DNA.

Targeting specific interactions to improve binding properties of EGFR-kinase ligands

248th National Meeting (2014)

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