2016-2017 Faculty Research Grant
Desmond Murray (Chemistry) and Denise Smith (Biology)
Hybrid Boronic Acids as Potential Antiglioblastoma Agents
The objective of this chemistry-biology collaborative research project is to investigate the synthesis and biological activity of hybrid boronic acids as potential antiglioblastoma agents. Glioblastomas are the most devastating of brain cancers. It is highly invasive, making surgical intervention less successful. Even though brain cancers account for a small percentage of all cancers, they account for a large number of deaths. Less than 10% of these cases will survive to five years. Therefore, the research community is seeking new therapeutics that targets glioblastomas.
Our approach is to develop and investigate hybrid boronic acids as potential agents against glioblastomas. In particular, we are exploring synthesis and antiglioblastoma testing of α-cyanostilbene boronic acids and heterocyclic arylidene boronic acids. The literature indicates that both α-cyanostilbenes and heterocyclic arylidenes show anticancer activity independently. The novelty of our approach is to covalently attach boronic acids to α-cyanostilbene and heterocyclic arylidene molecular ‘scaffolds’ to determine whether or not increased therapeutic potency is obtained. Part of our working hypothesis is that the boronic acid group would improve recognition of and attachment to the cancer cell surface via interactions with specific glycoproteins. Boronic acidcarbohydrate interactions is a well-established and documented phenomena but has not been applied as described in our proposal. As a consequence, our proposed antiglioblastoma agents could specifically and selectively target the cancer cells and facilitate mechanisms of action that lead to their apoptosis.