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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

Tasisulam sodium (LY573636-sodium): clinically evaluated (phase II/III in metastatic melanoma) antitumor N-acylsulfonamide; pan-Bcl family inhibitors targeting Bcl-2, Bcl-w, and Bcl-xL: WO-2002024636, ABT-737, and ABT-263 [23–25]
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Related In: Results  -  Collection


getmorefigures.php?uid=PMC4494775&req=5

Fig3: Tasisulam sodium (LY573636-sodium): clinically evaluated (phase II/III in metastatic melanoma) antitumor N-acylsulfonamide; pan-Bcl family inhibitors targeting Bcl-2, Bcl-w, and Bcl-xL: WO-2002024636, ABT-737, and ABT-263 [23–25]

Mentions: A number of structurally novel N-acylbenzenesulfonamides have recently been reported either as potent antitumor agents against a broad spectrum of human tumor xenografts (colon, lung, breast, ovary, and prostate) in nude mice [22] (Fig. 2) or clinically investigated drug candidates with cytostatic activity against malignant tumors such as Eli Lilly’s tasisulam sodium [23] or Abbott’s WO-2002024636, ABT-737 [24], and ABT-263 [25] (Fig. 3).Fig. 2


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)

Tasisulam sodium (LY573636-sodium): clinically evaluated (phase II/III in metastatic melanoma) antitumor N-acylsulfonamide; pan-Bcl family inhibitors targeting Bcl-2, Bcl-w, and Bcl-xL: WO-2002024636, ABT-737, and ABT-263 [23–25]
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4494775&req=5

Fig3: Tasisulam sodium (LY573636-sodium): clinically evaluated (phase II/III in metastatic melanoma) antitumor N-acylsulfonamide; pan-Bcl family inhibitors targeting Bcl-2, Bcl-w, and Bcl-xL: WO-2002024636, ABT-737, and ABT-263 [23–25]
Mentions: A number of structurally novel N-acylbenzenesulfonamides have recently been reported either as potent antitumor agents against a broad spectrum of human tumor xenografts (colon, lung, breast, ovary, and prostate) in nude mice [22] (Fig. 2) or clinically investigated drug candidates with cytostatic activity against malignant tumors such as Eli Lilly’s tasisulam sodium [23] or Abbott’s WO-2002024636, ABT-737 [24], and ABT-263 [25] (Fig. 3).Fig. 2

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