Molecular editing of kinase-targeting Resorcylic Acid Lactones (RAL): Fluoroenone RAL

Abstract

(Chemical Equation Presented) Molecular editing: The resorcylic acid lactones (RAL) are known small-molecule irreversible inhibitors of select kinases, and represent a unique pharmacophore with potential for further development in kinase research. The basic pharmacophore was "edited" to improve the properties and to diversify the scaffold. Two fluoroenones were synthesized, and their preliminary biological evaluation revealed interesting activity. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.