Regio- and stereoselective synthesis of 2'-β-substituted-fluoroneplanocin A analogues as potential anticancer agents

Org Biomol Chem. 2015 Sep 21;13(35):9236-48. doi: 10.1039/c5ob01348h. Epub 2015 Jul 30.

Abstract

A series of 2'-β-substituted-6'-fluoro-cyclopentenyl-pyrimidines and -purines 8 and 9 were successfully synthesized from d-ribose in a regio- and stereoselective manner. The functionalization at the C2-position of 6'-fluoro-cyclopentenyl nucleosides was achieved via regioselective protection of a hydroxyl group at the C3-position and stereoselective formation of C2-triflate followed by direct SN2 reaction with a fluoro or azido nucleophile. All the synthesized compounds were evaluated for their anticancer activities in several tumor cell lines, but were found to be neither active nor toxic.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / analogs & derivatives*
  • Adenosine / chemical synthesis
  • Adenosine / chemistry
  • Adenosine / pharmacology
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Chemistry Techniques, Synthetic
  • Humans
  • Stereoisomerism

Substances

  • Antineoplastic Agents
  • fluoroneplanocin A
  • Adenosine