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Pentamethinium salts as ligands for cancer: Sulfated polysaccharide co-receptors as possible therapeutic target
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SYSNO ASEP 0538135 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Pentamethinium salts as ligands for cancer: Sulfated polysaccharide co-receptors as possible therapeutic target Author(s) Bříza, T. (CZ)
Králová, Jarmila (UMG-J) RID
Rimpelová, S. (CZ)
Havlík, M. (CZ)
Kaplánek, R. (CZ)
Kejik, Z. (CZ)
Martásek, P. (CZ)
Mikula, I. (CZ)
Dzubak, P. (CZ)
Hajduch, M. (CZ)
Ruml, T. (CZ)
Král, V. (CZ)Number of authors 12 Source Title Bioorganic Chemistry. - : Elsevier - ISSN 0045-2068
Roč. 82, February (2019), s. 74-85Number of pages 12 s. Publication form Online - E Language eng - English Country US - United States Keywords Anticancer activity ; Cytotoxicity ; Fluorescent cyanine ; Pentamethinium salt ; Recognition ; Sulfated polysaccharides Subject RIV EB - Genetics ; Molecular Biology OECD category Cell biology R&D Projects LQ1604 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) ED1.1.00/02.0109 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) Method of publishing Limited access Institutional support UMG-J - RVO:68378050 UT WOS 000455479600009 DOI 10.1016/j.bioorg.2018.02.011 Annotation 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. (C) 2018 Published by Elsevier Inc. Workplace Institute of Molecular Genetics Contact Nikol Škňouřilová, nikol.sknourilova@img.cas.cz, Tel.: 241 063 217 Year of Publishing 2021 Electronic address https://www.sciencedirect.com/science/article/abs/pii/S0045206817306934?via%3Dihub
Number of the records: 1