Pentamethinium salts as ligands for cancer: Sulfated polysaccharide co-receptors as possible therapeutic target

. 2019 Feb ; 82 () : 74-85. [epub] 20180216

Jazyk angličtina Země Spojené státy americké Médium print-electronic

Typ dokumentu časopisecké články, práce podpořená grantem, audiovizuální média

Perzistentní odkaz   https://www.medvik.cz/link/pmid30273836
Odkazy

PubMed 30273836
DOI 10.1016/j.bioorg.2018.02.011
PII: S0045-2068(17)30693-4
Knihovny.cz E-zdroje

A series of pentamethinium salts with benzothiazolium and indolium side units comprising one or two positive charges were designed and synthesized to determine the relationships among the molecular structure, charge density, affinity to sulfated polysaccharides, and biological activity. Firstly, it was found that the affinity of the pentamethinium salts to sulfated polysaccharides correlated with their biological activity. Secondly, the side heteroaromates displayed a strong effect on the cytotoxicity and selectivity towards cancer cells. Finally, doubly charged pentamethinium salts possessing benzothiazolium side units exhibited remarkably high efficacy against a taxol-resistant cancer cell line.

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