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

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

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 1 , 2016

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Graphical 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.

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

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Article Details

Year: 2016
Published on: 30 October, 2015
Page: [77 - 88]
Pages: 12
DOI: 10.2174/1570180812666150611185830

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