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Design, synthesis, and in vitro evaluation of cytotoxic activity of new substituted 1,4-benzoquinones and hydroquinones

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Abstract

A new series of p-benzoquinones, hydroquinones, and quinol dimethyl ethers substituted by a pyrazole ring either directly or after an oxoethyl linker was synthesized and screened for in vitro cytotoxic activity. Compounds 8d, f, g, i, and 9c, f, and 13c exhibited broad-spectrum activity (GI50 MG-MID values 9.27–14.72 μM). With regard to sensitivity, compounds 8f and 9c, f have proved to possess a remarkable activity against leukemia tumor cell lines (GI50 = 3.43–5.03 μM). Indeed, compound 13c showed the highest activity profile against individual leukemia subpanel cell line SR (GI50 = 0.91 μM).

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Correspondence to Mona Mahran.

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Chaaban, I., EL-Khawass, ES., Mahran, M. et al. Design, synthesis, and in vitro evaluation of cytotoxic activity of new substituted 1,4-benzoquinones and hydroquinones. Med Chem Res 16, 49–77 (2007). https://doi.org/10.1007/s00044-007-9001-3

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  • DOI: https://doi.org/10.1007/s00044-007-9001-3

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