Synthesis and activity of staurosporine analogs with a lactone functionality

Abstract Staurosporine analogs, whose γ-lactam functionality was converted into γ-lactone, were synthesized. The key step involves remarkably efficient ring-opening and then intramolecular cyclization reactions. In general, those compounds display potent anti-platelet aggregation activity and show higher selectivity against platelet as compared with smooth muscle contraction.