Synthesis, Biological Screening, and Structure-Activity Relationships of Non-Proteinogenic Cyclic Hexapeptide Libraries

Combinatorial chemistry and high-throughput screening are indispensable tools used in chemical biology to synthesize diverse chemical libraries and identify potential drug leads.  Natural products and their derivatives have historically served as successful drug leads due to their structural complexity and co-evolution within biological systems. Components of natural product scaffolds may serve as beneficial motifs in the development of new biological probes.  The focus of this project is to synthesize a natural product-like peptide library and screen it for bioactivity against cancer cells.  The project will encompass several aspects of medicinal chemistry such as library design, organic synthesis, compound analysis, principles of screening, deconvolution strategies, and hit optimization.  Our efforts have the potential to lead to the discovery of promising new bioactive scaffolds.

Preferred Duration: 8 weeks

Mentor: Scott Lokey, Professor
Secondary Mentor: Mr. Andrew Bockus