A novel class of small-molecule caspase-3 inhibitors prepared by multicomponent reactions

► The MCR scope for the synthesis of pentasubstituted polyfunctional dihydropyrroles 6 were expanded. ► Tetra- and pentasubstituted dihydropyrroles 5 and 6 are a novel series of caspase-3 inhibitors. ► The inhibitory activity of 5 and 6 depend on the nature of substituents on different positions.