Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents

Grzegorz Cholewiński; Dorota Iwaszkiewicz-Grześ; Piotr Trzonkowski; Krystyna Dzierzbicka

doi:10.3109/14756366.2015.1077821

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)

Grzegorz Cholewiński dr hab. inż.
Dorota Iwaszkiewicz-Grześ mgr inż.
Piotr Trzonkowski
- Gdański Uniwersytet Medyczny Katedra Immunologii
Krystyna Dzierzbicka prof. dr hab. inż.
Dorota Iwaszkiewicz-Grzes

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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