简便半合成 Garcinoic 酸及其类似物并评估其对人源 DNA 聚合酶 β 的抑制作用。
A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β.
机构信息
Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA.
Department of Biochemistry and Molecular Biology, College of Medicine, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA.
出版信息
Molecules. 2020 Dec 11;25(24):5847. doi: 10.3390/molecules25245847.
Garcinoic acid has been identified as an inhibitor of DNA polymerase β (pol β). However, no structure-activity relationship (SAR) studies of garcinoic acid as a pol β inhibitor have been conducted, in part due to the lack of an efficient synthetic method for this natural product and its analogs. We developed an efficient semi-synthetic method for garcinoic acid and its analogs by starting from natural product δ-tocotrienol. Our preliminary SAR studies provided a valuable insight into future discovery of garcinoic acid-based pol β inhibitors.
garcinoic 酸已被鉴定为 DNA 聚合酶 β（pol β）的抑制剂。然而，garcinoic 酸作为 pol β 抑制剂的构效关系（SAR）研究尚未进行，部分原因是缺乏这种天然产物及其类似物的有效合成方法。我们从天然产物 δ-生育三烯醇开始，开发了 garcinoic 酸及其类似物的有效半合成方法。我们的初步 SAR 研究为未来发现基于 garcinoic 酸的 pol β 抑制剂提供了有价值的见解。
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