Halogenated 2-amino-4H-benzo[h]chromene derivatives as antitumor agents and the relationship between lipophilicity and antitumor activity

Several halogenated 2-amino-4 H -benzo[ h ]chromene derivatives were synthesized and evaluated their cytotoxicity. The structures of the synthesized compounds were established on the basis of spectral data. The in vitro antitumor activity of the synthesized compounds against the cell lines MCF-7, HCT-116, and HepG-2 was investigated in comparison with the reference drugs vinblastine, colchicine, and doxorubicin using microculture tetrazolium colorimetric assay. It was found that some halogenated 4 H -benzo[ h ]chromene derivatives showed the highest antitumor activity as compared with the reference drugs. The structure – activity relationship studies reported that the substitution at 4-position in the 4 H -benzo[ h ]chromene nucleus with the specific halogen groups and lipophilicity increases the ability of the molecule against the different cell lines.