当前位置: X-MOL 学术Bioorgan. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Pentamethinium salts as ligands for cancer: Sulfated polysaccharide co-receptors as possible therapeutic target
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2018-02-16 , DOI: 10.1016/j.bioorg.2018.02.011
Tomáš Bříza , Jarmila Králová , Silvie Rimpelová , Martin Havlík , Robert Kaplánek , Zdeněk Kejík , Pavel Martásek , Ivan Mikula , Petr Džubák , Marián Hajdúch , Tomáš Ruml , Vladimír Král

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.



中文翻译:

五甲亚锡盐作为癌症的配体:硫酸化多糖共受体可能是治疗目标

设计并合成了一系列带有苯并噻唑鎓和吲哚鎓侧链的,包含一个或两个正电荷的五甲亚铵盐,以确定分子结构,电荷密度,对硫酸化多糖的亲和力和生物活性之间的关系。首先,发现五次甲基鎓盐对硫酸化多糖的亲和力与其生物学活性有关。其次,侧杂芳酸酯显示出对癌细胞的细胞毒性和选择性的强烈影响。最后,具有苯并噻唑鎓侧单元的双电荷的五次甲基鎓盐对紫杉醇抗性癌细胞系显示出显着的高功效。

更新日期:2018-02-16
down
wechat
bug