Title:New Analogues of Mycophenolic Acid
Volume: 17
Issue: 9
Author(s): Agnieszka Siebert, Michal Prejs, Grzegorz Cholewinski*Krystyna Dzierzbicka
Affiliation:
- Faculty of Chemistry, Department of Organic Chemistry, Gdansk University of Technology, G. Narutowicza St 11/12, 80-233 Gdansk,Poland
Keywords:
Anticancer agents, antiproliferative activity, conjugates, immunosuppressants, IMPDH, Mycophenolic acid.
Abstract: Background: Mycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive
and anticancer properties. It is a non-competitive and reversible inhibitor of dehydrogenase
inosine-5'-monophosphate (IMPDH). This compound belongs to the immunosuppressive
drugs used for the prevention of both acute and chronic transplant rejection. Until now, two derivatives
of MPA have been used clinically: mycophenolate mofetil (MMF, CellCept) and mycophenolate sodium
(MPS, Myfortic). They cause, similar to MPA, although at lower degree, the side effects such as
vomiting, abdominal pain, diarrhea, nausea, gastrointestinal, urogenital tract, blood or nervous system
disorders. These drawbacks and glucuronidation of MPA in vivo limit the use of these compounds as
pharmaceuticals. Therefore, research is still going on for more effective analogs that are less toxic to
the organism and could improve the quality of life of patients.
Conclusion: In this review article, the authors present the synthesis of novel derivatives of mycophenolic
acid, together with their initial biological investigations.
