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Synthesis and in vitro activity of novel 2-(benzylthio)-4-chloro-5-(1,3,4-oxadiazol-2-yl)benzenesulfonamide derivatives.

Brożewicz K, Sławiński J - Monatsh. Chem. (2012)

Bottom Line: Two series of novel 4-chloro-2-(benzylthio)-5-(1,3,4-oxadiazol-2-yl)benzenesulfonamides and their N-aroyl derivatives have been synthesized and evaluated for in vitro anticancer activity against the full NCI-60 cell line panel.Most of the compounds exhibited antiproliferative activity.Among them a compound bearing an N-(thien-2-ylcarbonyl) moiety showed broad-spectrum activity with 50% growth inhibition (GI50) values in the range of 2.02-7.82 μM over 50 cell lines. .

View Article: PubMed Central - PubMed

Affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Al. Gen. J. Hallera 107, 80-416 Gdańsk, Poland.

ABSTRACT

Abstract: Two series of novel 4-chloro-2-(benzylthio)-5-(1,3,4-oxadiazol-2-yl)benzenesulfonamides and their N-aroyl derivatives have been synthesized and evaluated for in vitro anticancer activity against the full NCI-60 cell line panel. Most of the compounds exhibited antiproliferative activity. Among them a compound bearing an N-(thien-2-ylcarbonyl) moiety showed broad-spectrum activity with 50% growth inhibition (GI50) values in the range of 2.02-7.82 μM over 50 cell lines.

Graphical abstract: .

No MeSH data available.


Related in: MedlinePlus

Differential cytotoxicity graph for 2a and 2c revealing NCI-60 panel selectivity/resistance pattern expressed in % growth. Sulfonamides 2a and 2c show significant selectivity toward CCRF-CEM human T cell lymphoblast-like cell line. For each agent the difference between mean % growth and % growth of each cell line for that agent is determined, to yield positive values for cell lines more sensitive than average (bars projecting above the horizontal axis) and negative values for cell lines less sensitive than average (bars projecting below the horizontal axis). Mean graph midpoint (the origin of the abscissa) for 2a is 98.22% and for 2c is 92.12%
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Fig4: Differential cytotoxicity graph for 2a and 2c revealing NCI-60 panel selectivity/resistance pattern expressed in % growth. Sulfonamides 2a and 2c show significant selectivity toward CCRF-CEM human T cell lymphoblast-like cell line. For each agent the difference between mean % growth and % growth of each cell line for that agent is determined, to yield positive values for cell lines more sensitive than average (bars projecting above the horizontal axis) and negative values for cell lines less sensitive than average (bars projecting below the horizontal axis). Mean graph midpoint (the origin of the abscissa) for 2a is 98.22% and for 2c is 92.12%

Mentions: Compounds 2a–2d and 4a–4j submitted to National Cancer Institute (NCI) were evaluated for their in vitro anticancer activity. Sulfonamides 2a and 2c showed significant selectivity toward leukemia cell line CCRF-CEM (Fig. 4), whereas 2d appears to be substantially inactive.Fig. 4


Synthesis and in vitro activity of novel 2-(benzylthio)-4-chloro-5-(1,3,4-oxadiazol-2-yl)benzenesulfonamide derivatives.

Brożewicz K, Sławiński J - Monatsh. Chem. (2012)

Differential cytotoxicity graph for 2a and 2c revealing NCI-60 panel selectivity/resistance pattern expressed in % growth. Sulfonamides 2a and 2c show significant selectivity toward CCRF-CEM human T cell lymphoblast-like cell line. For each agent the difference between mean % growth and % growth of each cell line for that agent is determined, to yield positive values for cell lines more sensitive than average (bars projecting above the horizontal axis) and negative values for cell lines less sensitive than average (bars projecting below the horizontal axis). Mean graph midpoint (the origin of the abscissa) for 2a is 98.22% and for 2c is 92.12%
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Related In: Results  -  Collection

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Fig4: Differential cytotoxicity graph for 2a and 2c revealing NCI-60 panel selectivity/resistance pattern expressed in % growth. Sulfonamides 2a and 2c show significant selectivity toward CCRF-CEM human T cell lymphoblast-like cell line. For each agent the difference between mean % growth and % growth of each cell line for that agent is determined, to yield positive values for cell lines more sensitive than average (bars projecting above the horizontal axis) and negative values for cell lines less sensitive than average (bars projecting below the horizontal axis). Mean graph midpoint (the origin of the abscissa) for 2a is 98.22% and for 2c is 92.12%
Mentions: Compounds 2a–2d and 4a–4j submitted to National Cancer Institute (NCI) were evaluated for their in vitro anticancer activity. Sulfonamides 2a and 2c showed significant selectivity toward leukemia cell line CCRF-CEM (Fig. 4), whereas 2d appears to be substantially inactive.Fig. 4

Bottom Line: Two series of novel 4-chloro-2-(benzylthio)-5-(1,3,4-oxadiazol-2-yl)benzenesulfonamides and their N-aroyl derivatives have been synthesized and evaluated for in vitro anticancer activity against the full NCI-60 cell line panel.Most of the compounds exhibited antiproliferative activity.Among them a compound bearing an N-(thien-2-ylcarbonyl) moiety showed broad-spectrum activity with 50% growth inhibition (GI50) values in the range of 2.02-7.82 μM over 50 cell lines. .

View Article: PubMed Central - PubMed

Affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Al. Gen. J. Hallera 107, 80-416 Gdańsk, Poland.

ABSTRACT

Abstract: Two series of novel 4-chloro-2-(benzylthio)-5-(1,3,4-oxadiazol-2-yl)benzenesulfonamides and their N-aroyl derivatives have been synthesized and evaluated for in vitro anticancer activity against the full NCI-60 cell line panel. Most of the compounds exhibited antiproliferative activity. Among them a compound bearing an N-(thien-2-ylcarbonyl) moiety showed broad-spectrum activity with 50% growth inhibition (GI50) values in the range of 2.02-7.82 μM over 50 cell lines.

Graphical abstract: .

No MeSH data available.


Related in: MedlinePlus