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Antiproliferative Activity of Polyether Antibiotic--Cinchona Alkaloid Conjugates Obtained via Click Chemistry. 2015
Iwona Skiera, and
Michał Antoszczak, and
Justyna Trynda, and
Joanna Wietrzyk, and
Przemysław Boratyński, and
Karol Kacprzak, and
Adam Huczyński
Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61-614, Poznan, Poland.
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 3.00 μm) and appeared to be less toxic and more selective against normal cells than two standard anticancer drugs.
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