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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
1 Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia 2 Department of Drug Radiation Research, National Center for Radiation Research and Technology, Nasr City, Cairo 11371, Egypt
* Author to whom correspondence should be addressed.
Received: 23 February 2014 / Revised: 19 March 2014 / Accepted: 20 March 2014 / Published: 1 April 2014
(This article belongs to the Section Bioinorganic Chemistry)
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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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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.

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