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Abstract
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 Electronic supplementary materialThe online version of this article (doi:10.1007/s00706-012-0849-7) contains supplementary material, which is available to authorized users.
Highlights
The aryl- and heteroarylsulfonamides are widely described compounds revealing a broad spectrum of applications in biological and pharmacological areas [1]
A series of novel 4-chloro-N-(4,5-dihydro-5-oxo1-R2-1H-1,2,4-triazol-3-yl)-5-methyl-2-(R1-methylthio)benzenesulfonamide derivatives have been synthesized as potential anticancer agents
We have reported the synthesis and anticancer activity of 2-mercaptobenzenesulfonamides and subsequently extended our study to analogues with various heterocyclic ring systems attached to the benzenesulfonamide scaffold [4,5,6, 8, 10, 15] (Fig. 1 structure A [4,5,6, 8, 15], B [8], C [10])
Summary
The aryl- and heteroarylsulfonamides are widely described compounds revealing a broad spectrum of applications in biological and pharmacological areas [1]. 2-mercaptobenzenesulfonamide derivatives (MBSAs) have been of interest because of the various biological properties including antitumor [2,3,4,5,6,7,8,9,10], antimicrobial [11, 12], and antiviral activities [13, 14], and inhibition of carbonic anhydrase [15,16,17]. It has been known that aryl/heteroarylsulfonamides may act as antitumor agents through a variety of mechanisms such as cell cycle perturbation in the G1 phase, disruption of microtubules, angiogenesis inhibition, and functional suppression of the transcriptional activator NF-Y. We have reported the synthesis and anticancer activity of 2-mercaptobenzenesulfonamides and subsequently extended our study to analogues with various heterocyclic ring systems attached to the benzenesulfonamide scaffold [4,5,6, 8, 10, 15] (Fig. 1 structure A [4,5,6, 8, 15], B [8], C [10])
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