Synthesis of spirooxindole-O-naphthoquinone-tetrazolo[1,5-a]pyrimidine hybrids as potential anticancer agents

Abstract

A series of novel spirooxindole-O-naphthoquinone-tetrazolo[1,5-a]pyrimidine hybrids were designed, synthesized and evaluated as potent antitumor agents. These hybrids exhibited relatively high cytotoxic activity against cancer cell line HepG2 (IC50 = 2.86-36.34 µM), while normal cell line LO2 was less sensitive to these hybrids (IC50 = 36.37-248.39 µM). On the whole, among all the compounds tested, compound 4e, with a mean IC50 value of 2.86 µM, was the most active. The novel hybrids may find their pharmaceutical applications after further investigations.