Kinases are enzyme catalysts that allow the transfer of phosphate from ATP to serine, threonine, and tyrosine amino acids of their respective substrate proteins. Although a large number of kinases have been discovered, the biological roles of the majority of these kinases remain unknown. This along with the fact that kinase inactivity has been strongly correlated to a number of human diseases has propelled research into better understanding kinase activity and developing small molecules that target these proteins. Success in targeting kinases is underscored by the fact that there are more than sixty FDA-approved kinase inhibitor drugs, and many studies have demonstrated that protein kinases are one of the most effective protein targets for drug therapeutics.<br/>Despite the breakthroughs in recent years, kinase potential still remains largely untapped, and a number of calls for contribution have been made. To answer this call, a composition of a public library of kinase activity, called the kinase chemogenomic set (KCGS), was recently disclosed to accelerate the synthesis and screening of drugs targeting kinase activity. With public access to the KCGS, many researchers are leveraging this resource to study biological function and therapeutic potential of many understudied kinases. As a part of this public effort, our group has focused on the synthesis of a benzoxazole compound that targets CK2, a human kinase whose upregulation is associated with several forms of cancer. In developing a procedure for the synthesis of drugs targeting this kinase, we hope to develop a library of potent and selective compounds that can later be screened as potential treatments for human diseases and added to the comprehensive public library of kinase inhibitors.

Synthesis of benzoxazole inhibitors targeting kinase CK2

ACS Spring 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.