Multicomponent reactions have been employed for the rapid preparation of potent kinase inhibitors against multiple kinase targets. We capitalized on the ability of MCRs to generate unique and underexplored chemical space around kinase hinges for the dual purpose of obtaining novel new inhibitors and thoroughly explore the ATP-competitive binding site of kinases. The compounds prepared were evaluated against a panel of kinase assays and potent inhibitors were identified for Gsk3b, Rock2 and EgfrFigure 1.  Design of novel molecules based on known kinase hinges

MCRS: A rapid and efficient way of exploring chemical space around kinase hinge binders to identify potent kinase inhibitors

243rd National Meeting (2012)

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