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

International Journal of Molecular Sciences

Mostafa M. Ghorab¹  Marwa G. El-Gazzar² 

[1] Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia; E-Mail:;Department of Drug Radiation Research, National Center for Radiation Research and Technology, Nasr City, Cairo 11371, Egypt; E-Mail:

关键词: sulfonamides;    heterocycles;    structure-activity relationships;    antitumor agents;   

DOI  :  10.3390/ijms15045582

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland