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, 1H NMR, 13C NMR and MS data. The invitro
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 4Hbenzo[
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.
Keywords: 4H-Benzo[h]chromenes, 7H-Benzo[h]chromeno[2, 3-d]pyrimidines, antitumor, SAR, molecular docking.
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