2. Academic Validation
  3. Cytotoxic effects of kinetin riboside and its selected analogues on cancer cell lines

Cytotoxic effects of kinetin riboside and its selected analogues on cancer cell lines

  • Bioorg Med Chem Lett. 2024 Mar 1:100:129628. doi: 10.1016/j.bmcl.2024.129628.
Ewa Totoń 1,  Natalia Lisiak 2,  Aleksandra Romaniuk-Drapała 2,  Grzegorz Framski 3,  Eliza Wyszko 3,  Tomasz Ostrowski 4
Affiliations

Affiliations

  • 1 Department of Clinical Chemistry and Molecular Diagnostics, Poznan University of Medical Sciences, Rokietnicka 3, 60-806 Poznan, Poland. Electronic address: etoton@ump.edu.pl.
  • 2 Department of Clinical Chemistry and Molecular Diagnostics, Poznan University of Medical Sciences, Rokietnicka 3, 60-806 Poznan, Poland.
  • 3 Institute of Bioorganic Chemistry, Polish Academy of Sciences, Noskowskiego 12/14, 61-704 Poznan, Poland.
  • 4 Institute of Bioorganic Chemistry, Polish Academy of Sciences, Noskowskiego 12/14, 61-704 Poznan, Poland. Electronic address: tostr@ibch.poznan.pl.
PMID: 38280656 DOI: 10.1016/j.bmcl.2024.129628
Abstract

N6-[(Furan-2-yl)methyl]adenosine (kinetin riboside) and its seven synthesized analogues were examined for the ability to inhibit the growth of five human carcinoma cell lines and for comparison of normal human lung fibroblast cell line (MRC-5). Out of the compounds evaluated, 8-azakinetin riboside was shown to exhibit significant cytotoxic activity for 72 h treatment against ovarian OVCAR-3 and pancreatic MIA PaCa-2 Cancer cells (IC50 = 1.1 μM) with an observed weaker effect against MRC-5 cells (IC50 = 4.6 μM). Kinetin riboside, as well as its N6-[(furan-3-yl)methyl]- and N6-[(thien-2-yl)methyl]- counterparts, also exhibited cytotoxic activities at low micromolar levels but were non-selective over MRC-5 cells.

Keywords

Cytokinin riboside; Cytotoxic activity; Modified nucleoside; Selectivity; Structure-activity relationship.

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