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Abstract
The group of new amide derivatives of mycophenolic acid (MPA) and selected heterocyclic amines was synthesised as potential immunosuppressive agents functioning as inosine-5'-monophosphate dehydrogenase (IMPDH) uncompetitive inhibitors. The synthesis employed uronium-type activating system (TBTU/HOBt/DIPEA) while or phosphonic acid anhydride method (T3P/Py) facilitating amides to be obtained in moderate to excellent yields without the need of phenolic group protection. Most of optimised protocols did not require complicated reaction work-ups, including chromatographic, solvent- consuming methods. The biological activity assay was performed on the T-Jurkat cell line and peripheral mononuclear blood cells (PBMCs) which are both dedicated for antiproliferative activity determination. Each of designed derivatives was characterised by reduced cytotoxicity and benzoxazole analogue revealed the most promising activity. Subsequently, an observed structure-activity relationship was discussed.
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Authors (7)
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Dorota Iwaszkiewicz-Grześ Dr
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Michalina Ziomkowska mgr inż.
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Piotr Trzonkowski
Cite as
Full text
- Publication version
- Accepted or Published Version
- DOI:
- Digital Object Identifier (open in new tab) 10.1080/14756366.2022.2127701
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- Category:
- Articles
- Type:
- artykuły w czasopismach
- Published in:
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JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
no. 37,
pages 2725 - 2741,
ISSN: 1475-6366 - Language:
- English
- Publication year:
- 2022
- Bibliographic description:
- Walczak J., Iwaszkiewicz-Grześ D., Ziomkowska M., Śliwka-Kaszyńska M., Daśko M., Trzonkowski P., Cholewiński G.: Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents// JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY -Vol. 37,iss. 1 (2022), s.2725-2741
- DOI:
- Digital Object Identifier (open in new tab) 10.1080/14756366.2022.2127701
- Sources of funding:
-
- Statutory activity/subsidy
- Verified by:
- Gdańsk University of Technology
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