Synthesis and anti-breast cancer evaluation of novel N-(guanidinyl)benzenesulfonamides

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A series of 4-(substituted)-N-(guanidinyl)benzenesulfonamides bearing biologically active pyrazole, pyrimidine and pyridine moieties were prepared and evaluated for their anticancer activity against human tumor breast cell line (MCF7). These sulfonamides showed promising activity with IC 50 values ranging from 49.5 to 70.2 μM. The structure-activity relationship of the synthesized compounds was studied. Interestingly, it was found that the most potent compounds in this study were the corresponding 2-cyanoacrylate 3, 3-oxobutanoate 4, pyrazole 6, pyridine 9 and pyrazole 13. Compounds 7 and 8 are nearly as active as Doxorubicin as reference drug with (IC 50 values = 70.2, 68.1 μM), while compounds 5, 10 and 11 exhibited a moderate activity. © 2014 by the authors; licensee MDPI, Basel, Switzerland.




Ghorab, M. M., El-Gazzar, M. G., & Alsaid, M. S. (2014). Synthesis and anti-breast cancer evaluation of novel N-(guanidinyl)benzenesulfonamides. International Journal of Molecular Sciences, 15(4), 5582–5595.

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