Ontology highlight
ABSTRACT:
SUBMITTER: Huber K
PROVIDER: S-EPMC3257585 | biostudies-literature | 2012 Jan
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20120103 1
Development of both potent and selective kinase inhibitors is a challenging task in modern drug discovery. The innate promiscuity of kinase inhibitors largely results from ATP-mimetic binding to the kinase hinge region. We present a novel class of substituted 7,8-dichloro-1-oxo-β-carbolines based on the distinct structural features of the alkaloid bauerine C whose kinase inhibitory activity does not rely on canonical ATP-mimetic hinge interactions. Intriguingly, cocrystal structures revealed an ...[more]