Abstract
In the present study, novel derivatives of 7H-benzo[h]chromeno[2,3-d]pyrimidine were prepared from 4H-benzo[h]chromene-3-carbonitrile and ethyl 4H-benzo[h]chromene-3-carboxylate derivatives and were evaluated as potential cytotoxic agents. The structures of the synthesized compounds were established on the basis of spectral data, IR, H-1 NMR, C-13 NMR and MS data. The in-vitro antitumor activity of the synthesized compounds was investigated in comparison with the standard drug Colchicine using MTT colorimetric assay. We explored the Structure-Activity Relationship (SAR) of 4H-benzo[h]chromenes with modification at the 2- or 3-positions and 2,3-positions. It was found that some compounds showed good antitumor activity against the cell lines MCF-7, HCT-116 and HepG-2 as compared with Colchicine. The SAR study revealed that the antitumor activity of the synthesized compounds were significantly affected by the lipophilicity (hydrophobic or hydrophilic) of the substituent at 2- or 3-positions and 2,3-positions.