Kinase Inhibitors

About

Summary Dr. Paul Wender and his colleague at Stanford have developed novel routes to new ATP binding site inhibitors that are useful as kinase inhibitors, and also as starting materials and/or intermediates in synthesizing other kinase inhibitors. Kinase inhibitors are used to treat diseases such as cancer, atherosclerosis, diabetes, CNS disorders and autoimmune diseases. Some are progressing in clinical trials. In particular, tyrosine kinases (TKs) have been associated with cell proliferation, activation or differentiation, and excessive TK activity has been observed in many disease states including benign and malignant proliferative disorders and immune system disorders. Certain TKs have also been identified as mediators of angiogenesis and are involved in the progression of cancer and other diseases involving inappropriate vascularization. Dr. Wender's analogs are highly potent, are readily synthesized from simple starting materials and are being tuned to selectively inhibit specific kinases. The route to these novel analogs involves a new and as yet unpublished multicomponent cascade reaction that allows quick access to drug-like structures. Applications As novel lead compounds and drug candidates for the treatment of conditions, diseases and disorders that are responsive to protein kinase inhibitors i.e., cancer, atherosclerosis, diabetes, CNS disorders and autoimmune diseases. Advantages Highly potent Readily synthesized from simple starting materials using straightforward synthetic chemistry Can be selectively modified to inhibit a particular kinase