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.
Mini-Reviews in Medicinal Chemistry
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.Export Options
About this article
Cite this article as:
Siebert Agnieszka, Prejs Michal, Cholewinski Grzegorz*, Dzierzbicka Krystyna, New Analogues of Mycophenolic Acid, Mini-Reviews in Medicinal Chemistry 2017; 17 (9) . https://dx.doi.org/10.2174/1389557516666161129160001
DOI https://dx.doi.org/10.2174/1389557516666161129160001 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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