1345018-87-2Relevant academic research and scientific papers
Synthesis and cytotoxicity of some d-mannose click conjugates with aminobenzoic acid derivatives
Hradilová, Ludmila,Poláková, Monika,Dvo?áková, Barbora,Hajdúch, Marián,Petru?, Ladislav
, p. 1 - 6 (2013/01/15)
Two sets of new conjugates obtained from d-mannose derivatives and o-, m-, and p-substituted benzoic acid esters interconnected through a triazole ring were synthesized by Cu(I) catalyzed azide-alkyne cycloaddition. All synthesized compounds were tested for their in vitro cytotoxic activity against seven cancer cell lines with/without multidrug resistance phenotype as well as non-tumor MRC-5 and BJ fibroblasts. Butyl ester of 4-aminobenzoic acid 6c showed the highest activity among all tested compounds, however, it was active only against K562 myeloid leukemia cells. N-Glycosyltriazole conjugates, both acetylated and nonacetylated at mannose moiety, were almost completely inactive. In contrast, some of the acetylated O-glycosyl conjugates showed cytotoxic activity which was cell line dependent and strongly affected by position of benzoic acid substitution as well as a length of its ester alkyl chain; the most potent compound was acetylated mannoside conjugated with octyl ester of m-substituted benzoic acid. However, deacetylation resulting in hydrophilicity increase of the glycosides almost completely abolished their cytotoxic potency.
Design, synthesis and biological evaluation of mannosyl triazoles as FimH antagonists
Schwardt, Oliver,Rabbani, Said,Hartmann, Margrit,Abgottspon, Daniela,Wittwer, Matthias,Kleeb, Simon,Zalewski, Adam,Smie?ko, Martin,Cutting, Brian,Ernst, Beat
experimental part, p. 6454 - 6473 (2011/12/14)
Urinary tract infection (UTI) caused by uropathogenic Escherichia coli (UPEC) is one of the most prevalent infectious diseases. Particularly affected are women, who have a 40-50% risk to experience at least one symptomatic UTI episode at some time during
