Cytotoxic activity of some novel sulfonamide derivatives.

Ghorab, M. M., M. S. Alsaid, M. S. Alsaid, and R. K. Arafa, "Cytotoxic activity of some novel sulfonamide derivatives.", Acta poloniae pharmaceutica, vol. 72, issue 1, pp. 79-87, 2015 Jan-Feb.


The versatile synthons 2-chloro-N-(4-sulfamoylphenyl)acetamides la,b were used as a key intermediates for the synthesis of sulfonamide derivatives with adamantyl 2, indene 3, morpholinophenyl 4, pipronyl 5, benzothiazole 6-8, pyrazole 9, thiadiazole 10,11, quinoline 12, isoquinoline 13, thiazoles 14-19, acrylamides 20-24 and benzochromene 25 moieties via reaction with several nitrogen nucleophiles. The newly synthesized compounds were screened in vitro for their anticancer activity against breast cancer (MDA-MB-231) and colon cancer (HT-29) cell lines. Compound 17 was found to be the most potent against breast cancer cell lines with IC55 value 66.6 μM compared with the reference drug 5-fluorouracil with IC50 value 77.28 μM.