The identification and advancement of early hit compounds to promising leads and beyond in drug discovery depends on a synergy among synthetic chemistry development, medicinal chemistry optimization and biology expertise. Our group has focused on deriving unique, drug-like structural architecture that can be leveraged to study intricate cellular pathways and discover new therapeutic opportunities. The methodologies pioneered in our lab have been used to assemble a proprietary compound library that is rigorously maintained, tracked and assessed across diverse assay platforms in partnership with a network of skilled biologists representing virology, parasitology, bacteriology, cancer mechanisms, and metabolic and neurologic diseases. Early results emerging from the screening of some of these new scaffolds will be discussed, and a mature project will be highlighted that demonstrates the pivotal role that synthetic chemistry has played in defining a pharmacophore and engineering a modified scaffold worthy of preclinical evaluation.

Development of novel transformations and structural templates to fuel medicinal chemistry discovery and optimization

2019 Spring National Meeting

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