Anti-proliferative activity of Monensin and its tertiary amide derivatives

  • Bioorg Med Chem Lett. 2015 Oct 15;25(20):4539-43. doi: 10.1016/j.bmcl.2015.08.067.
Adam Huczyński  1 ,  Greta Klejborowska  2 ,  Michał Antoszczak  2 ,  Ewa Maj  3 ,  Joanna Wietrzyk  3
Affiliations
  • 1. Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89 b, 61-614 Poznań, Poland. Electronic address: [email protected].
  • 2. Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89 b, 61-614 Poznań, Poland.
  • 3. Ludwik Hirszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Rudolfa Weigla 12, 53-114 Wrocław, Poland.
PMID: 26338363 DOI: 10.1016/j.bmcl.2015.08.067
Abstract

New tertiary amide derivatives of polyether ionophore Monensin A (MON) were synthesised and their anti-proliferative activity against Cancer cell lines was studied. Very high activity (IC50=0.09 μM) and selectivity (SI=232) of MON against human biphenotypic myelomonocytic leukemia cell line (MV4-11) was demonstrated. The MON derivatives obtained exhibit interesting anti-proliferative activity, high selectivity index and also are able to break the drug-resistance of Cancer cell line.

Keywords
Anti-proliferative activity; Natural products; Polyether ionophores; Selectivity; Tertiary amides.