二糖核苷类似物的合成及其作为潜在多聚（ADP-核糖）聚合酶-1 抑制剂的研究。
Synthesis of disaccharide nucleoside analogues as potential poly(ADP-ribose) polymerase-1 inhibitors.
机构信息
Department of Chemistry and Konstanz Research School Chemical Biology, University of Konstanz, Universitätsstraße 10, 78457 Konstanz, Germany.
出版信息
Org Biomol Chem. 2018 Nov 28;16(46):8904-8907. doi: 10.1039/c8ob01894d.
PMID:30203829
Abstract
Poly(ADP-ribose) polymerase-1 (PARP-1) is an important target in cancer therapy. We present the synthesis of novel disaccharide nucleoside analogues that resemble the central motif of poly(ADP-ribose) and test their inhibitory effects on human PARP-1. Some compounds show inhibition of enzymatic activity in vitro and thus might be interesting for further investigations.
摘要
聚（ADP-核糖）聚合酶-1（PARP-1）是癌症治疗的一个重要靶点。我们合成了类似聚（ADP-核糖）核心结构的新型二糖核苷类似物，并测试了它们对人 PARP-1 的抑制作用。一些化合物在体外显示出对酶活性的抑制作用，因此可能值得进一步研究。
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