SEMINAR: Bayliss Seminar Series

The application of small molecules for the modulation of large biomacromolecules has seen much research in the last decades. This includes molecules capable of interfering with phosphate-transfer proteins such as kinases and phosphatases. These proteins have been identified as being of importance in many therapeutic processes, particularly in the treatment of cancer. The targeted inactivation of this class of enzymes is critical as it is important to differentiate between the inhibition of normal and unwanted cellular processes (such as uncontrolled cell growth and division).

In recent years, the value of the covalent inhibition of biological targets has seen a resurgence, with particular success being achieved in terms of kinase targets. In addition, the fairly recent “rediscovery” of (metal-mediated) click reactions, and their application in medicinal chemistry initiatives, has also provided interesting opportunities. In this presentation, our approaches to the design and synthesis of novel small molecule kinase inhibitors, making use of a combination of irreversible inhibition and “click” synthetic strategies, will be described.