519053-87-3Relevant articles and documents
Syntheses of a new series of N-amino-N′-(benzenesulphonyl)guanidine derivatives with potential antitumor activity
Slawinski,Bednarski,Gruenert,Reszka
, p. 53 - 64 (2007/10/03)
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 (5b) (IC50 = 2.35-8.14 μM) and 3-phenylamino-1-(4-chloro-2-ethoxycarbonylmethylthio-5- methylbenzenesulphonyl)guanidine (5c) (IC50 = 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.