Diversity Orientated Synthesis

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SELECTBIO

Modern advances in chemical biology include the improvement of screening methods, the introduction of bioinformatics methods to unravel biological pathways, and the development of high-quality chemical libraries. In this view, Diversity-Oriented Synthesis (DOS) gathered interest to explore systematically the chemical space by generating small-molecule collections as probes to investigate biological pathways. DOS consists of synthesizing structurally diverse compounds from a complexity-generating reaction followed by cyclization steps and appendage diversity. Also, chemical genetics emerged as a tool in chemical biology for its role in selecting small molecules capable to induce a biological phenotype or to interact with a gene product. Our efforts in this field are focused on the production of diversity-oriented molecules of peptidomimetic nature as tool addressing protein-protein interactions, taking advantage of amino acid- and sugar-derived polyfunctional building blocks to be applied in couple-pair synthetic approaches. We are applying such peptidomimetic scaffolds to biological evaluation using cell growth as a phenotypic screening on yeast deletant strains to identify hit compounds in the discovery of novel antifungal and anticancer agents, and to dissect their mode of action.