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Deoxynucleosides with benzimidazoles as aglycone moiety are potent anticancer agents

Mirosława Koronkiewicz1, Zdzisław Chilmonczyk1, Zygmunt Kazimerczuk2

  • 1Department of Cell Biology, National Medicines Institute, Chełmska St. 30/34, 00-725 Warsaw, Poland.

European Journal of Pharmacology
|December 17, 2017
PubMed

Insights

New deoxynucleoside compounds targeting CK2 and PIM-1 kinases show promise as anticancer agents. These inhibitors effectively induce apoptosis in cancer cells, offering potential for targeted therapy in myeloid leukemia and prostate cancer.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Elevated levels of CK2 and PIM-1 serine/threonine kinases are linked to cancer development.
  • These kinases suppress apoptosis, protecting cancer cells from death.
  • Inhibiting these kinases can promote cancer cell apoptosis.

Purpose of the Study:

  • To evaluate the in vitro anticancer activity of novel protein kinase inhibitors.
  • To explore the efficacy of deoxynucleosides with tetrahalobenzimidazole aglycones against neoplastic cells.

Main Methods:

  • Synthesis and testing of deoxynucleoside derivatives.
  • Flow cytometry to assess cytotoxicity, apoptosis induction, and cell cycle.
  • Measurement of mitochondrial membrane potential and caspase activity.

Main Results:

  • Compounds, including K164 (TDB), demonstrated varied cytotoxicity and proapoptotic effects.
  • The tested inhibitors effectively induced apoptosis in cancer cell lines.
  • Mechanism of action studies provided insights into their anticancer properties.

Conclusions:

  • The studied deoxynucleoside derivatives are potential anticancer agents.
  • These compounds show particular promise for targeted therapy in myeloid leukemia and prostate cancer.
  • Further research is warranted to explore their therapeutic potential.
Keywords:
Anticancer effectsFlow cytometryProtein kinase inhibitorsTetrahalobenzimidazoles

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