Abstract

Extracellular signal-regulated kinase 5 (ERK5) plays a key role in the transduction of extracellular signals to intracellular effectors. Activation of the ERK5 signalling pathway is associated with cell survival and proliferation, and thus ERK5 over-expression has implications in carcinogenesis. Inhibiting ERK5 is therefore an effective approach for anti-cancer therapy. Following a high throughput screening campaign, three chemical series (1 -3) were selected for validation. The syntheses and biological evaluation of novel benzo[d]thiazoles (1), 4-aminopyrimidine-5-carbonitriles (2) and 3 cyanopyridines (3) will be discussed.