Indolylmaleimides, derived from staurosporine, is a specific class of protein kinase C inhibitors. The structure modification, synthesis and biological activity of indolylmaleimide derivatives have been reviewed in this paper. The main parts were focused on the introduction of the synthetic routes. Both merits and limitations of the synthetic methods have been discussed.

Key words: protein kinase C inhibitor, indolylmaleimide, structure modification, biological activity, synthesis