The mitogen activated protein kinase (MAPK) pathway is a family of interrelated signal transduction kinases involved in complex signaling events mediating cell differentiation, proliferation, and death. Extracellular mitogen or ligand binding begins a signaling cascade that activates MEK resulting in phosphorylation of its corresponding and specific ERK substrate (extracellular signal-regulated kinase). ERK-5 is the only known substrate of MEK-5. The MEK-5/ERK-5 pathway is involved in cell survival, anti-apoptotic signaling, angiogenesis, and cell motility. MEK-5 is significantly up regulated in specific cancers including breast and prostate cancers. We synthesized a series of diphenylamines based on a revised homology model of MEK5 based on the X-ray crystal structure of MEK-1 (PDB ID: 3EQC). Synthesis and biological evaluation of novel amide and aryl variations will be presented. 

Synthesis and biological evaluation of selective MEK-5 inhibitors

244th National Meeting (2012)

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