Expanding molecular diversity with pseudopeptides and macrotorials: Synthesis, characterization, and biological activities of macrocyclic combinatorial libraries

Abstract

Combinatorial mixtures represent a potentially rich source of drug leads if problems involving deconvolution and structure optimization can be overcome. Cyclic peptides and their analogs are partially constrained systems that reduce the complexities inherent with linear macromolecules. Through careful optimization of synthetic procedures, we have been able to prepare, test, and interpret biological results from both small and large (>1000 component) cyclic peptide libraries.