Design and synthesis of oridonin derivatives as cytotoxic agents

IF 1.9 3区 化学 Q3 CHEMISTRY, APPLIED Natural Product Research Pub Date : 2025-02-01 DOI:10.1080/14786419.2023.2275287
Chen-Liang Zhao , Chi-Yuan Zhang , Xiao-Min Yang , Ka Hei Lam , Yi-Xuan Xia , Yin-Xiao Du , Lu-Tai Pan , Hong-Jie Zhang
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Abstract

Oridonin is one of the ent-kaurane diterpenes that have been studied extensively for various bioactivities. In an effort to expand natural scaffold-based library as anticancer agents, we have designed and synthesised a number of novel oridonin derivatives and evaluated their bioactivities on a panel of human cancer cell lines (HCT116, A375, MCF-7, HepG2, and A549). Compound 4b bearing a 4-fluorophenyl moiety was found to be the most active compound with an IC50 value of 0.3 μM against MCF-7 cells, which was 7.4-fold more active than oridonin. This study could provide some insightful information for further synthesis of oridonin derivatives as anticancer agents.
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冬凌草甲素衍生物的设计和合成。
冬凌草甲素是一种具有多种生物活性的铀烷二萜。为了扩大天然支架库作为抗癌剂,我们设计并合成了许多新型冬凌草甲素衍生物,并在一组人类癌症细胞系(HCT116、A375、MCF-7、HepG2和A549)上评估了它们的生物活性。发现带有4-氟苯基部分的化合物4b是IC50值为0.3的最具活性的化合物 μM对抗MCF-7细胞,其活性是冬凌草甲素的7.4倍。该研究可为进一步合成冬凌草甲素衍生物作为抗癌剂提供一些有见地的信息。
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来源期刊
Natural Product Research
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.
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