Synthesis, Cytotoxicities and DNA-Binding Affinities of Benzofuran-3-ols and Their Fused Analogs

Abstract

A series of benzofuropyrazoles 2a—i were synthesized in 10—92% from the reaction of 2-aroylbenzofuran-3-ols 1a—i with hydrazine hydrate, and screened for their antitumor activities toward four human solid tumor cell lines, including gastric carcinoma cells MKN45, hepatocellular carcinoma cells HepG2, breast cancer cells MCF-7, and lung cancer cells A549. The results indicated that both compounds 1a—i and 2a—i displayed moderate antitumor activities. Among them, compound 2e exhibited potent inhibitory activity toward all the four tumor cell lines. In addition, compounds 1e and 2e showed strong DNA-binding affinities, and induced an increase in the viscosity of calf-thymus DNA, suggesting that they might act as an intercalator.