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New Analogues of Mycophenolic Acid

[ Vol. 17 , Issue. 9 ]

Author(s):

Agnieszka Siebert, Michal Prejs, Grzegorz Cholewinski* and Krystyna Dzierzbicka   Pages 734 - 745 ( 12 )

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.

Keywords:

Anticancer agents, antiproliferative activity, conjugates, immunosuppressants, IMPDH, Mycophenolic acid.

Affiliation:

Department of Organic Chemistry, Gdansk University of Technology, Narutowicza St 11/12, PL 80-233 Gdansk, Department of Organic Chemistry, Gdansk University of Technology, Narutowicza St 11/12, PL 80-233 Gdansk, Faculty of Chemistry, Department of Organic Chemistry, Gdansk University of Technology, G. Narutowicza St 11/12, 80-233 Gdansk, Department of Organic Chemistry, Gdansk University of Technology, Narutowicza St 11/12, PL 80-233 Gdansk

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