Journal
MINI-REVIEWS IN MEDICINAL CHEMISTRY
Volume 17, Issue 9, Pages 734-745Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1389557516666161129160001
Keywords
Anticancer agents; antiproliferative activity; conjugates; immunosuppressants; IMPDH; Mycophenolic acid
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Funding
- Polish National Science Center (NCN) [2013/11/B/NZ7/04838, DS 031832]
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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.
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