Synthesis and antiproliferative activity of new mycophenolic acid conjugates with adenosine derivatives

J Asian Nat Prod Res. 2019 Feb;21(2):178-185. doi: 10.1080/10286020.2018.1451521. Epub 2018 Apr 2.

Abstract

New conjugates of mycophenolic acid (MPA) and adenosine derivatives were synthesized and assessed as potential immunosuppressants on Jurkat cell line and peripheral blood mononuclear cells (PBMC) from healthy donors. As compared to MPA, all compounds were found to be more active against Jurkat cell line. The antiproliferative activities were compared with MPA and adenosine, in both 2',3'-O-isopropylidene protected and free hydroxyl groups possessing forms. The obtained results were also discussed in terms of selectivity index, defined as SI = IC50/EC50.

Keywords: Mycophenolic acid; adenosine derivatives; antiproliferative activity; esterification.

MeSH terms

  • Adenosine / analogs & derivatives*
  • Adenosine / chemical synthesis*
  • Adenosine / chemistry
  • Adenosine / pharmacology
  • Cell Proliferation / drug effects
  • Humans
  • Immunosuppressive Agents / chemical synthesis*
  • Immunosuppressive Agents / pharmacology*
  • Jurkat Cells
  • Mycophenolic Acid / analogs & derivatives*
  • Mycophenolic Acid / chemical synthesis*
  • Mycophenolic Acid / chemistry
  • Mycophenolic Acid / pharmacology

Substances

  • Immunosuppressive Agents
  • Mycophenolic Acid
  • Adenosine