The design, synthesis and activity of non-ATP competitive inhibitors of pp60c-src tyrosine kinase.Part 1: Hydroxynaphthalene derivatives

A series of hydroxynaphthalene pp60c-src non-peptide inhibitors was designed, using the crystal structure of the insulin receptor tyrosine kinase as a qualitative model, to target the peptide substrate binding site. Representative inhibitors were shown to bind non-competitively with respect to ATP.