Syntheses of a New Series of N‐Amino‐N′‐(benzenesulfonyl)guanidine Derivatives with Potential Antitumor Activity.

doi:10.1002/CHIN.200325114

Paper

Syntheses of a New Series of N‐Amino‐N′‐(benzenesulfonyl)guanidine Derivatives with Potential Antitumor Activity.

Published Jun 24, 2003 · J. Sławiński, P. Bednarski, R. Gruenert

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Abstract

Syntheses of novel N-amino-N'-(benzenesulphonyl)guanidines (4a-h, 5a-g) from N-(benzenesulphonyl)cyanamide potassium salt and hydrazine derivatives are described. Compounds 4b, 5a-c and 5e were evaluated by in vitro assays of growth inhibition against several human tumor cell lines. The highest in vitro cytotoxic activities were found for 3-phenylamino-1-(2-benzylthio-4-chloro-5-methylbenzenesulphonyl)guanidine (Sb) (IC 5 0 = 2.35-8.14 μM) and 3-phenylamino-1-(4-chloro-2-ethoxycarbonylmethyl-thio-5-methylbenzenesulphonyl)guanidine (5c) (IC 5 0 = 2.74-10.6 μM), while other tested compounds (5a, 5e) showed the moderate cytotoxic activities.The molecular orbital calculation of the possible tautomeric forms of the benzenesulphonylguanidine derivatives were also presented.

In Vitro Study

Study Snapshot

The novel N-amino-N'-(benzenesulphonyl)guanidine derivatives show potential antitumor activity, with 3-phenylamino-1-(2-benzylthio-4-chloro-5-methylbenzenesulphonyl)guanidine

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Syntheses of a New Series of N‐Amino‐N′‐(benzenesulfonyl)guanidine Derivatives with Potential Antitumor Activity.

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