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Synthesis and biological activity of mycophenolic acid-amino acid derivatives

Abstract

In search of new immunosuppressants, mycophenolic acid (MPA) was coupled with amino acid methyl esters followed by hydrolysis to analogs bearing free carboxylic groups. The obtained compunds were tested in vitro as growth inhibitors of lymphoid cell line (Jurkat) and human peripheral blood mononuclear cells (PBMC) from healthy donors. According to obtained results recovering of free carboxylic group increased their activity. Additionally, the cytotoxic properties depends on the substituent and configuration at chiral center in amino acid unit. Three derivatives revealed higer potency than parent MPA.

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Details

Category:
Articles
Type:
artykuł w czasopiśmie wyróżnionym w JCR
Published in:
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY no. 69, pages 863 - 871,
ISSN: 0223-5234
Language:
English
Publication year:
2013
Bibliographic description:
Iwaszkiewicz-Grześ D., Cholewiński G., Kot-Wasik A., Trzonkowski P., Dzierzbicka K.: Synthesis and biological activity of mycophenolic acid-amino acid derivatives// EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. -Vol. 69, (2013), s.863-871
Verified by:
Gdańsk University of Technology

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