The corner stone of drug discovery has been firmly rooted within natural products, which have been, and continue to be the dominant force in therapeutic agent discovery. The lasting impact of natural products is continually felt by this field, even today. However, given the current decline in the discovery of new natural products possessing potent cytotoxicity, and the advancement of robotics in the 1990’s via high-throughput screening, an urgent need of screening compounds has become a “call-to-arms” by the synthetic community. One answer to this call was via robust sp2-sp2 coupling chemistry to provide access to large commercially available chemical screening libraries, but these lack in structural complexity and complex biological activity. Others have used various means at obtaining new compounds for screening collections, such as: epigenetics, diversity orientated synthesis (DOS) and functional diversity synthesis. Our laboratory has focused upon the construction of new classes of targeted and designed screening libraries based upon the synthetically amendable and versatile intermediates within total synthesis routes. Through these untapped small molecules, our laboratory has discovery new drug delivery systems, new potent bioactive small molecules, and developed new chemical screening libraries. Said libraries have allowed for investigations into molecule transport across gram-negative bacteria and the blood-brain barrier. To be presented will be the application of our penetrant chaperones and new biologically relevant small molecules.

Discovery of new bioactive small molecules and approaches at new chemical screening libraries

255th National Meeting (2018)

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