Antiproliferative Activity of Polyether Antibiotic - Cinchona Alkaloid Conjugates Obtained via Click Chemistry

作者:Skiera Iwona; Antoszczak Michal; Trynda Justyna; Wietrzyk Joanna; Boratynski Przemyslaw; Kacprzak Karol*; Huczynski Adam
来源:Chemical Biology & Drug Design, 2015, 86(4): 911-917.
DOI:10.1111/cbdd.12523

摘要

A series of eight new conjugates of salinomycin or monensin and Cinchona alkaloids were obtained by the Cu(I)-catalysed 1,3-dipolar Huisgen cycloaddition (click chemistry) of respective N-propargyl amides of salinomycin or monensin with four different Cinchona alkaloid derived azides. In vitro antiproliferative activity of these conjugates evaluated against three cancer cell lines (LoVo, LoVo/DX, HepG2) showed that four of the compounds exhibited high antiproliferative activity (IC50 below 3.00m) and appeared to be less toxic and more selective against normal cells than two standard anticancer drugs.

  • 出版日期2015-10