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Synthesis and Anticancer Activity of Dimeric Polyether Ionophores
Michał Sulik1, Ewa Maj2, Joanna Wietrzyk2
1Department of Medical Chemistry, Faculty of Chemistry, Adam Mickiewicz University, Uniwersytetu Poznańskiego 8, 61-614 Poznań, Poland.
Biomolecules
|July 16, 2020
Summary
New dimeric polyether ionophores show enhanced anticancer activity, selectively targeting various cancer cells and overcoming drug resistance. These novel compounds offer promising therapeutic potential against diverse malignancies.
Area of Science:
- Natural Products Chemistry
- Medicinal Chemistry
- Oncology
Background:
- Polyether ionophores possess broad bioactivity, including anticancer properties.
- Salinomycin, lasalocid acid, and monensin are key ionophores targeting cancer cells, including cancer stem cells.
- Multivalent structures of ionophores remain underexplored for therapeutic applications.
Purpose of the Study:
- To synthesize novel homo- and heterodimeric polyether ionophores.
- To evaluate the antiproliferative activity of synthesized dimers against various cancer cell lines.
- To investigate the potential of these dimers in overcoming drug resistance.
Main Methods:
- Synthesis of salinomycin homo- and heterodimers using triazole linkers.
- Synthesis of 'mixed' dimers combining salinomycin with lasalocid acid, monensin, or betulinic acid.
- In vitro antiproliferative assays against six cancer cell lines, including a doxorubicin-resistant line.
Main Results:
- Eleven novel dimeric compounds were synthesized and characterized.
- Five dimers demonstrated superior antiproliferative potency compared to parent compounds and cytostatic drugs.
- Two dimers effectively overcame doxorubicin resistance in the LoVo/DX colon adenocarcinoma cell line.
Conclusions:
- Dimeric polyether ionophores represent a promising class of anticancer agents.
- These novel structures exhibit enhanced selectivity and potency against various cancer types.
- The synthesized dimers hold potential for overcoming multidrug resistance in cancer therapy.
