3-和5-β-去斑蝥素偶联物的合成。

IF 1.9 3区化学 Q3 CHEMISTRY, APPLIED

Natural Product Research Pub Date : 2025-02-01 DOI:10.1080/14786419.2023.2269466

Han Lin , Weiwei Dong , Changkuo Zhao , Xianheng Wang

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引用次数: 0

摘要

利用分子杂交技术开发天然抗肿瘤药物缀合物是近年来药物开发的研究热点之一。本研究将具有抗癌活性的β-无氢羊藿碱选择性地与去甲斑蝥啶偶联，以开发新的抗肿瘤先导物。在EDCI/DMAP/DCM条件下，将β-无氢羊藿碱的C-3和C-5羟基分别与去甲斑蝥素单酸酯偶联，采用CCK-8法检测合成的偶联物对HepG2、MCF-7和L-02细胞的抑制活性。这些结合物对HepG2和MCF-7细胞系的抑制活性均优于亲本化合物去斑蝥素，但弱于亲本化合物去斑蝥素。

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Synthesis of 3- and 5-β-anhydroicaritine norcantharidin conjugates

Using molecular hybridisation to develop conjugates of natural antitumor drugs is one of the research hotspots in recent drug development. In this study, β-anhydroicaritine with anticancer activity was conjugated to norcantharidine selectively to develop new antitumor lead candidates. In the condition of EDCI/DMAP/DCM, the C-3 and C-5 hydroxyl groups of β-anhydroicaritine was coupled with norcantharidin monoacid ester respectively, and the inhibitory activity of the synthesised conjugates against HepG2, MCF-7 and L-02 cells were tested by CCK-8 method. Most of these conjugates showed a better activity against HepG2 and MCF-7 cell lines compared to parent compound icaritin, but weaker than another parent compound norcantharidin.

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来源期刊

Natural Product Research 化学-医药化学

CiteScore

5.10

自引率

9.10%

发文量

605

审稿时长

2.1 months

期刊介绍： The aim of Natural Product Research is to publish important contributions in the field of natural product chemistry. The journal covers all aspects of research in the chemistry and biochemistry of naturally occurring compounds. The communications include coverage of work on natural substances of land and sea and of plants, microbes and animals. Discussions of structure elucidation, synthesis and experimental biosynthesis of natural products as well as developments of methods in these areas are welcomed in the journal. Finally, research papers in fields on the chemistry-biology boundary, eg. fermentation chemistry, plant tissue culture investigations etc., are accepted into the journal. Natural Product Research issues will be subtitled either ""Part A - Synthesis and Structure"" or ""Part B - Bioactive Natural Products"". for details on this , see the forthcoming articles section. All manuscript submissions are subject to initial appraisal by the Editor, and, if found suitable for further consideration, to peer review by independent, anonymous expert referees. All peer review is single blind and submission is online via ScholarOne Manuscripts.