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Int. J. Mol. Sci. 2014, 15(4), 5582-5595; doi:10.3390/ijms15045582
Article

Synthesis and Anti-Breast Cancer Evaluation of Novel N-(Guanidinyl)benzenesulfonamides

1,* , 2
 and 1
Received: 23 February 2014; in revised form: 19 March 2014 / Accepted: 20 March 2014 / Published: 1 April 2014
(This article belongs to the Section Biochemistry, Molecular Biology and Biophysics)
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Abstract: 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 IC50 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 (IC50 values = 70.2, 68.1 μM), while compounds 5, 10 and 11 exhibited a moderate activity.
Keywords: sulfonamides; heterocycles; structure-activity relationships; antitumor agents sulfonamides; heterocycles; structure-activity relationships; antitumor agents
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Ghorab, M.M.; El-Gazzar, M.G.; Alsaid, M.S. Synthesis and Anti-Breast Cancer Evaluation of Novel N-(Guanidinyl)benzenesulfonamides. Int. J. Mol. Sci. 2014, 15, 5582-5595.

AMA Style

Ghorab MM, El-Gazzar MG, Alsaid MS. Synthesis and Anti-Breast Cancer Evaluation of Novel N-(Guanidinyl)benzenesulfonamides. International Journal of Molecular Sciences. 2014; 15(4):5582-5595.

Chicago/Turabian Style

Ghorab, Mostafa M.; El-Gazzar, Marwa G.; Alsaid, Mansour S. 2014. "Synthesis and Anti-Breast Cancer Evaluation of Novel N-(Guanidinyl)benzenesulfonamides." Int. J. Mol. Sci. 15, no. 4: 5582-5595.


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