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Novel 5'-Norcarbocyclic Derivatives of Bicyclic Pyrrolo- and Furano[2,3-d]Pyrimidine Nucleosides.

Anna A KlimenkoElena S MatyuginaEvgeniya B LogashenkoPavel N SolyevMarina A ZenkovaSergey N KochetkovAnastasia L Khandazhinskaya
Published in: Molecules (Basel, Switzerland) (2018)
Here we report the synthesis and biological activity of new 5'-norcarbocyclic derivatives of bicyclic pyrrolo- and furano[2,3-d]pyrimidines with different substituents in the heterocyclic ring. Lead compound 3i, containing 6-pentylphenyl substituent, displays inhibitory activity with respect to a number of tumor cells with a moderate selectivity index value. Compound 3i induces cell death by the apoptosis pathway with the dissipation of mitochondrial potential.
Keyphrases
  • cell death
  • cell cycle arrest
  • oxidative stress
  • structure activity relationship
  • endoplasmic reticulum stress
  • high intensity
  • human health
  • risk assessment