Three-component coupling of 3-amino-1,2,4-triazole, aldehydes and 3-hydroxy-8- methyl-1,4-phenanthrenequinone has been achieved using a catalytic amount of p-TsOH under solvent-free conditions to produce a novel series of tanshinone I derivatives having azacyclo in good yields and with high regioselectivity. These compounds are found to exhibit potent antitumoral properties.