Recent advances in the discovery of Src kinase inhibitors

Src family kinases are involved in the regulation of a wide variety of normal cellular signal transduction pathways, such as cell growth, differentiation, survival, adhesion and migration. Considerable evidence implicates elevated expression and/or activity of Src kinases in many human cancers, osteoporosis, cardiovascular disorders and immune system dysfunction; thus, this family of protein tyrosine kinases now exists as intriguing targets for both basic research and drug discovery. Herein, a number of examples of currently developed Src family kinase inhibitors in selected patents from 2002 – 2005 will be described. Special attention will be made to the chemical diversity of ATP binding site inhibitors, potency, selectivity and therapeutic application of the compounds.