新型麦考酚酸与腺苷衍生物缀合物的合成及其抗增殖活性
Synthesis and antiproliferative activity of new mycophenolic acid conjugates with adenosine derivatives.
作者信息
Prejs Michał, Cholewiński Grzegorz, Trzonkowski Piotr, Kot-Wasik Agata, Dzierzbicka Krystyna
机构信息
a Department of Organic Chemistry , Gdansk University of Technology , Gdansk PL 80-233 , Poland.
b Department of Clinical Immunology and Transplantology , Medical University of Gdansk , Gdansk 80-211 , Poland.
出版信息
J Asian Nat Prod Res. 2019 Feb;21(2):178-185. doi: 10.1080/10286020.2018.1451521. Epub 2018 Apr 2.
New conjugates of mycophenolic acid (MPA) and adenosine derivatives were synthesized and assessed as potential immunosuppressants on Jurkat cell line and peripheral blood mononuclear cells (PBMC) from healthy donors. As compared to MPA, all compounds were found to be more active against Jurkat cell line. The antiproliferative activities were compared with MPA and adenosine, in both 2',3'-O-isopropylidene protected and free hydroxyl groups possessing forms. The obtained results were also discussed in terms of selectivity index, defined as SI = IC/EC.
合成了霉酚酸（MPA）与腺苷衍生物的新型缀合物，并评估了其对Jurkat细胞系和健康供体外周血单个核细胞（PBMC）作为潜在免疫抑制剂的活性。与MPA相比，所有化合物对Jurkat细胞系的活性更高。比较了2',3'-O-异丙叉基保护型和游离羟基型的抗增殖活性与MPA和腺苷的抗增殖活性。还根据选择性指数（定义为SI = IC/EC）对所得结果进行了讨论。
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