NA - IDENTIFICATION OF NEW TUBULIN INHIBITORS USING IN SITU CLICK CHEMISTRY

Cancer is an important public health concern around the world. Chemotherapy is no doubt one of the most successful ways in which cancer can be treated, but still there exist a need for new cancer agents. In this research proposal we will apply in situ cli ck chemistry for the identification of new tubulin inhibitors that may offer a new approach to cancer chemotherapy. Professor K. B. Sharpless and co-workers at The Scripps Research Institute have recently introduced click chemistry as a tool in drug disc overy. Click chemistry was their response to the problems associated with making reliable libraries of potential lead structures in medicinal chemistry using combinatorial chemistry. Click chemistry is a modular approach to chemical synthesis that utilize s only the most practical and reliable chemical transformations. Click chemistry is applied in two different ways: generation of target-specific compound libraries (combinatorial chemistry) and target-templated synthesis of inhibitors (in situ click chemi stry). The latter approach will enable faster discovery of lead molecules for development of new cancer agents.