Synthesis, Biological Evaluation and Molecular Docking Studies of 4Hbenzo[ h]chromenes, 7H-benzo[h]chromeno[2,3-d]pyrimidines as Antitumor Agents

Title:Synthesis, Biological Evaluation and Molecular Docking Studies of 4Hbenzo[ h]chromenes, 7H-benzo[h]chromeno[2,3-d]pyrimidines as Antitumor Agents

Volume: 13 Issue: 1

Author(s): Ahmed H. Halawa, Ahmed M. Fouda, Al-Anood M. Al-Dies and Ahmed M. El-Agrody

Affiliation:

Keywords: 4H-Benzo[h]chromenes, 7H-Benzo[h]chromeno[2, 3-d]pyrimidines, antitumor, SAR, molecular docking.

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, 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.

Cite this article as:

H. Halawa Ahmed, M. Fouda Ahmed, M. Al-Dies Al-Anood and M. El-Agrody Ahmed, Synthesis, Biological Evaluation and Molecular Docking Studies of 4Hbenzo[ h]chromenes, 7H-benzo[h]chromeno[2,3-d]pyrimidines as Antitumor Agents, Letters in Drug Design & Discovery 2016; 13 (1) . https://dx.doi.org/10.2174/1570180812666150611185830