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去氧五味子素的简洁全合成及其抗增殖作用及结构相关衍生物的探索。

A concise total synthesis of deoxyschizandrin and exploration of its antiproliferative effects and those of structurally related derivatives.

机构信息

Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, UK.

出版信息

Chemistry. 2012 Mar 12;18(11):3193-8. doi: 10.1002/chem.201103530. Epub 2012 Feb 3.

DOI:10.1002/chem.201103530
PMID:22307955
Abstract

The natural product deoxyschizandrin has been shown to have a wide range of biological activities. In recent years the therapeutic potential of this compound against cancers has attracted significant interest. Herein we describe a concise de novo total synthesis of deoxyschizandrin based around a double organocuprate oxidation strategy. In addition, we present the results of biological studies exploring the ability of deoxyschizandrin and synthetic precursors lacking the medium ring biaryl unit to inhibit the proliferation of a human cancer cell line. These studies led to the identification of a structurally novel agent with in vitro anticancer activity.

摘要

天然产物五味子素具有广泛的生物活性。近年来,该化合物在癌症治疗方面的潜力引起了广泛关注。本文描述了一种基于双有机铜试剂氧化策略的简洁的五味子素全合成方法。此外,我们还介绍了生物研究的结果,这些研究探索了五味子素和缺乏中环联芳烃单元的合成前体抑制人癌细胞系增殖的能力。这些研究确定了一种具有体外抗癌活性的结构新颖的药物。

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