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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
Abstract
Improved derivatives of mycophenolic acid (MPA) are necessary to reduce the frequency of adverse effects, this drug exerts in treated patients. In this study, MPA was coupled with N-(x-hydroxyalkyl)-9-acridone-4-carboxamides or N-(x-hydroxyalkyl)acridine-4-carboxamides to give respective ester conjugates upon Yamaguchi protocol. This esterification required protection of phenol group in MPA. Designed conjugates revealed higher potency in vitro than parent MPA. Acridine derivatives were more active than acridone analogs and length of the alkyl linker between MPA and heterocyclic units influenced the observed cytotoxicity.
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Authors (5)
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Piotr Trzonkowski
- Gdański Uniwersytet Medyczny Katedra Immunologii
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- Accepted or Published Version
- DOI:
- Digital Object Identifier (open in new tab) 10.3109/14756366.2015.1077821
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- Category:
- Articles
- Type:
- artykuł w czasopiśmie wyróżnionym w JCR
- Published in:
-
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
no. 31,
edition 6,
pages 974 - 982,
ISSN: 1475-6366 - Language:
- English
- Publication year:
- 2016
- Bibliographic description:
- Cholewiński G., Iwaszkiewicz-Grześ D., Trzonkowski P., Dzierzbicka K.: Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents// JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. -Vol. 31, iss. 6 (2016), s.974-982
- DOI:
- Digital Object Identifier (open in new tab) 10.3109/14756366.2015.1077821
- Verified by:
- Gdańsk University of Technology
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