, Volume 143, Issue 12, pp 1705-1718,
Open Access This content is freely available online to anyone, anywhere at any time.
Date: 25 Sep 2012

Synthesis and molecular structure of novel 2-(alkylthio)-4-chloro-N-(4,5-dihydro-5-oxo-1H-1,2,4-triazol-3-yl)-5-methylbenzenesulfonamides with potential anticancer activity


A series of novel 4-chloro-N-(4,5-dihydro-5-oxo-1-R2-1H-1,2,4-triazol-3-yl)-5-methyl-2-(R1-methylthio)benzenesulfonamide derivatives have been synthesized as potential anticancer agents. The in vitro antitumor activity of some compounds was evaluated in the US National Cancer Institute (NCI) against the NCI-60 cell line panel. The most prominent compound showed remarkable activity against 13 human tumor cell lines representing lung, colon, CNS, melanoma, ovarian, renal, prostate, and breast at low micromolar GI50 level in the range of 1.9–3.0 μM.

Graphical Abstract