Synthesis of several 4H-chromene derivatives of expected antitumor activity

Abstract

Multi-component reactions for the preparation of 4H-chromene derivatives under microwave irradiation from different aromatic aldehydes with a mixture of malononitrile and phenol derivatives were established. The cytotoxic activity of the target compounds was evaluated against four cancer cell lines MCF-7, HCT-116, HepG-2 and A549 in comparison with vinblastine and colchicine as reference drugs. Generally, several compounds showed good cell growth inhibitory activity as compared to standard drugs. The structure–activity relationship studies reported that the substitution at 4- and 6-positions in 4H-chromene nucleus with the specific halogen atom increases the ability of the molecule against the different cell lines. The structures of the synthesized compounds were established on the basis of spectral data, IR, 1H NMR, 13C NMR and MS data.