A series of 6‐(pyrrolyl) coumarin/quinolone derivatives have been synthesized in moderate to good yields (53‐79%) via one‐pot three‐component reactions of 6‐amino coumarin/quinolones, β‐nitrostyrenes and dialkyl acetylenedicarboxylates catalyzed by indium(III) chloride under microwave heating conditions.

A series of (1,5‐disubstituted 1,2,3‐triazolyl)coumarin/quinolone derivatives (tcd and tqd) have been synthesized in good to excellent yields via Ag2O NPs catalyzed azide‐alkyne cycloaddition reactions. We then tested the drug‐likeness of tcd and tqd by analyzing molecular descriptors. Rational drug design showed that these derivatives indeed are potential anticancer agents against tankyrases.