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

Ghorab, Mostafa M.; El-Gazzar, Marwa G.; Alsaid, Mansour S.

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.

BENZENESULFONAMIDES; ANTINEOPLASTIC agents; DRUG synthesis; PYRAZOLES; HETEROCYCLIC compounds synthesis; BREAST cancer treatment; STRUCTURE-activity relationships

International Journal of Molecular Sciences, 2014, Vol 15, Issue 4, p5582

1661-6596

Academic Journal

10.3390/ijms15045582