title: New conjugates of mycophenolic acid and their antiproliferative activity.
abstract: The new conjugates of mycophenolic acid (MPA) were obtained in the reaction of N(6)-(ω-aminoalkyl)adenosines with MPA in the presence of EDCI as a coupling reagent. New compounds 4a-h were evaluated on leukemia cell line (Jurkat) and PBMC from healthy donors. Length of the linker influenced observed activity. The compound 4b possessing 1,3-diamine spacer exhibited the most promising results and can be considered to further investigations.
authors.affiliation: a Department of Organic Chemistry , Gdansk University of Technology , 80-233 Gdansk , Poland.
authors.forename: Michał
authors.initials: M
authors.lastname: Prejs
authors.affiliation: a Department of Organic Chemistry , Gdansk University of Technology , 80-233 Gdansk , Poland.
authors.forename: Grzegorz
authors.initials: G
authors.lastname: Cholewinski
authors.affiliation: a Department of Organic Chemistry , Gdansk University of Technology , 80-233 Gdansk , Poland.
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Siebert
authors.affiliation: b Department of Clinical Immunology and Transplantology , Medical University of Gdansk , 80-211 Gdansk , Poland.
authors.forename: Piotr
authors.initials: P
authors.lastname: Trzonkowski
authors.affiliation: a Department of Organic Chemistry , Gdansk University of Technology , 80-233 Gdansk , Poland.
authors.forename: Krystyna
authors.initials: K
authors.lastname: Dzierzbicka
mesh_terms: D000241:Adenosine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D007963:Leukocytes, Mononuclear; D015394:Molecular Structure; D009173:Mycophenolic Acid / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D009173:Mycophenolic Acid; D000241:Adenosine
keywords: MPA; Mycophenolic acid; adenosine; antiproliferative activity; synthesis