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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.

Sławiński J, Żołnowska B, Orlewska C, Chojnacki J - Monatsh. Chem. (2012)

Bottom Line: A series of novel 4-chloro-N-(4,5-dihydro-5-oxo-1-R(2)-1H-1,2,4-triazol-3-yl)-5-methyl-2-(R(1)-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.

View Article: PubMed Central - PubMed

Affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Gen. J. Hallera Str. 107, 80416 Gdańsk, Poland.

ABSTRACT

Abstract: A series of novel 4-chloro-N-(4,5-dihydro-5-oxo-1-R(2)-1H-1,2,4-triazol-3-yl)-5-methyl-2-(R(1)-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.

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Sch1:   

Mentions: The main goal of this study was to synthesize and investigate the anticancer activity of the new 2-(alkylthio)benzenesulfonamides containing diverse substituted 1,2,4-triazol-5-one moieties. Thus, we propose a synthetic route leading to the target 2-(alkylthio)-4-chloro-N-(4,5-dihydro-5-oxo-1-R2-1H-1,2,4-triazol-3-yl)-5-methylbenzenesulfonamides as shown in Scheme 1.Scheme 1


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.

Sławiński J, Żołnowska B, Orlewska C, Chojnacki J - Monatsh. Chem. (2012)

  
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4495025&req=5

Sch1:   
Mentions: The main goal of this study was to synthesize and investigate the anticancer activity of the new 2-(alkylthio)benzenesulfonamides containing diverse substituted 1,2,4-triazol-5-one moieties. Thus, we propose a synthetic route leading to the target 2-(alkylthio)-4-chloro-N-(4,5-dihydro-5-oxo-1-R2-1H-1,2,4-triazol-3-yl)-5-methylbenzenesulfonamides as shown in Scheme 1.Scheme 1

Bottom Line: A series of novel 4-chloro-N-(4,5-dihydro-5-oxo-1-R(2)-1H-1,2,4-triazol-3-yl)-5-methyl-2-(R(1)-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.

View Article: PubMed Central - PubMed

Affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Gen. J. Hallera Str. 107, 80416 Gdańsk, Poland.

ABSTRACT

Abstract: A series of novel 4-chloro-N-(4,5-dihydro-5-oxo-1-R(2)-1H-1,2,4-triazol-3-yl)-5-methyl-2-(R(1)-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.

No MeSH data available.


Related in: MedlinePlus