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Extended Abstract

Double Modification of Polyether Ionophores: Synthesis and Biological Activity of Novel Salinomycin Derivatives †

by
Michał Antoszczak
1,*,
Dominika Czerwonka
1,
Alicja Urbaniak
2,
Szymon Sobczak
3,
Timothy C. Chambers
2 and
Adam Huczyński
1
1
Department of Bioorganic Chemistry, Faculty of Chemistry, Adam Mickiewicz University, 61–614 Poznań, Poland
2
Department of Biochemistry and Molecular Biology, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA
3
Department of Materials Chemistry, Faculty of Chemistry, Adam Mickiewicz University, 61–614 Poznań, Poland
*
Author to whom correspondence should be addressed.
†
Presented at the 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery, Barcelona, Spain, 15–17 May 2019.
Proceedings 2019, 22(1), 20; https://doi.org/10.3390/proceedings2019022020
Published: 7 August 2019
(This article belongs to the Proceedings of The 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery)
Versions Notes
Polyether ionophore antibiotics represent a large group of more than 120 lipid-soluble compounds that are widely used in veterinary medicine because of their significant antimicrobial activity. In addition to the industrial use of ionophores, some of them effectively and selectively inhibit properties of different cancer cells and enhance the antitumor effects of chemo- and/or radiotherapy. Salinomycin (SAL) is particularly interesting in this regard, as it shows potent activity against various types of cancer cells, including those that display multidrug resistance, and cancer stem cells. Therefore, a very interesting direction of research is chemical modification of SAL which may lead to obtaining analogs that are characterized by better biological activity and lower toxicity than those of the starting compound.
Within the library of SAL analogs investigated, its C1 and C20 derivatives have shown noteworthy improvements in the biological activity profile. Moreover, our previous studies support the double-modification of SAL as a useful strategy to generate agents with promising biological activity profiles for targeting various types of cancer. For example, it has been proven that the activity of double-modified SAL analogs can surpass commonly used cytostatic drugs in the multidrug resistant cancer cell lines. Here, we report the synthetic access to novel class of C1/C20 doubly modified SAL derivatives, and we present the results of the evaluation of their biological activity.

Acknowledgments

M.A. wishes to acknowledge the Polish Science Centre (NCN) for financial support by grant SONATA (2016/23/D/ST5/00242) and the Foundation for Polish Science (FNP) for a scholarship START.
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations.

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MDPI and ACS Style

Antoszczak, M.; Czerwonka, D.; Urbaniak, A.; Sobczak, S.; Chambers, T.C.; Huczyński, A. Double Modification of Polyether Ionophores: Synthesis and Biological Activity of Novel Salinomycin Derivatives. Proceedings 2019, 22, 20. https://doi.org/10.3390/proceedings2019022020

AMA Style

Antoszczak M, Czerwonka D, Urbaniak A, Sobczak S, Chambers TC, Huczyński A. Double Modification of Polyether Ionophores: Synthesis and Biological Activity of Novel Salinomycin Derivatives. Proceedings. 2019; 22(1):20. https://doi.org/10.3390/proceedings2019022020

Chicago/Turabian Style

Antoszczak, Michał, Dominika Czerwonka, Alicja Urbaniak, Szymon Sobczak, Timothy C. Chambers, and Adam Huczyński. 2019. "Double Modification of Polyether Ionophores: Synthesis and Biological Activity of Novel Salinomycin Derivatives" Proceedings 22, no. 1: 20. https://doi.org/10.3390/proceedings2019022020

APA Style

Antoszczak, M., Czerwonka, D., Urbaniak, A., Sobczak, S., Chambers, T. C., & Huczyński, A. (2019). Double Modification of Polyether Ionophores: Synthesis and Biological Activity of Novel Salinomycin Derivatives. Proceedings, 22(1), 20. https://doi.org/10.3390/proceedings2019022020

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