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Synthesis, in-vitro cytotoxicity of 4H-benzo[h]chromene derivatives and structure–activity relationships of 4-aryl group and 3-, 7-positions

Ahmed M. El-Agrody, Heba K. Abd El-Mawgoud, Ahmed M. Fouda, and Essam S. A. E. H. Khattab

Chemistry Department, Faculty of Science, Al-Azhar University, Nasr City 11884, Cairo, Egypt



Abstract: A series of 2-amino-4H-benzo[h]chromene and 2,7-diamino-4H-benzo[h]chromene derivatives were prepared as potential cytotoxic agents. The structures of the synthesised compounds were established on the basis of spectral data. The in-vitro cytotoxic activity of the synthesised compounds against the cell lines MCF-7, HCT-116 and HepG-2 was investigated in comparison with vinblastine and colchicine, using an MTT colorimetric assay. The structure-activity relationship of 4H-benzo[h]chromenes with modification at the 3-, 4- and 7-positions was explored. The results of the anti-tumour evaluation revealed that compounds VIIIc, VIId, VIIb, VIIe, VIIIg and VIIIc, VIId, VIIb, VIIe, VIIIg, VIIc, VIIIe, Vf, IIIa inhibited the growth of MCF-7 in comparison with vinblastine and colchicine, while VIIb, VIId, VIIe, IIIa, VIIa, VIIIc, VIIc, IIId, IIIg, IIIf, IIIb, IIIh, VIIIb, VIIIa, VIIIe, IIIc, Vg, IIIe, VIIIg, Vf, IIIf inhibited the growth of HCT-116 in comparison with colchicine. In addition, compounds VIIe, IIIg, IIIa, VIIc and VIIe, IIIg, IIIa, VIIc, VIIb, VIIa, VIIIf, VIIIe inhibited the growth of HepG-2 in comparison with vinblastine and colchicine, respectively.

Keywords: 1-naphthol – 5-amino-1-naphthol – 4H-benzo[h]chromenes – cytotoxicity – SAR

Full paper is available at

DOI: 10.1515/chempap-2016-0049


Chemical Papers 70 (9) 1279–1292 (2016)

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