Synthesis and biological evaluation of diaromatic guanidinium-like derivatives as protein kinase inhibitors for the treatment of cancer

Abstract

The aim of a chemotherapeutic drug is to specifically target a biomolecule involved in the development of cancer whilst not affecting healthy tissues. Unfortunately, this is a difficult task due to the complexity of the biochemical processes and regulatory mechanisms entailed. Targeting systems which are only up-regulated or mutated in cancer cells can help to achieve selectivity. A quintessential example of this approach is inhibiting the protein kinase family, which are enzymes involved in the pathophysiology of cancer. Their activity is regulated in normal cells; however, they are often over-expressed or mutated in cancer cells, leading to malfunctioning of signaling networks.