Synthesis of Spirooxindole-<em>O</em>-Naphthoquinone-Tetrazolo[1,5-<em>a</em>]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.

Keywords

• spirooxindole
• <i>O</i>-naphthoquinone
• hybrids
• antitumor activity