文摘
FLT3 kinase inhibitors are currently under investigation asa new treatment for acute myeloid leukemia. We report here a molecularconcept invoking interactions between an aromatic ring and the sidechains of Phe691 and Cys828, two residues of the ATP pocket, to obtainpotent and specific inhibitors of this kinase. The hypothesis has beenvalidated by the successful design of a new inhibitor prototype showingpromising antiproliferative activity in cellular assays.