Multicomponent one-pot synthesis of 2-naphthol derivatives and evaluation of their anticancer activity

Treatment of 2-naphthol with aldehydes and allyl tributyl stannane or anisole in the presence of AlCl3 at 0A degrees C to room temperature afforded its 1-alkyl derivatives in high yields (76-83%) within 4-8 h. The products were evaluated for their cytotoxic activity against four human cancer cell lines. The most potent compound (5d) showed IC50 of 1.2 +/- A 1.1, 1.6 +/- A 1.0, 0.9 +/- A 0.1, and 0.8 +/- A 0.4 mu M against Hep G(2), A549, MDA 231, and HeLa cell lines, respectively, and its activity was found to be comparable to that of doxorubicin. A new multicomponent synthesis of 2-naphthol derivatives has been developed. The cytotoxic activity of one of the 2-naphthol derivatives (A:R = 4-F-C6H5) was comparable to that of doxorubicin.