一种新型双联苄衍生物的合成及抗肿瘤活性

刘德秀; 潘华英; 石慧; 黄晓英; 娄红祥

doi:10.11665/j.issn.1000-5048.20130605

一种新型双联苄衍生物的合成及抗肿瘤活性

1.
苏州卫生职业技术学院
2.
山东大学药学院

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- 刊出日期: 2013-12-24

Synthesis and antitumor activity of a novel bisbibenzyl derivative

摘要

摘要: 以3，4-二甲氧基-6-溴苯甲醛、3-羟基-4-甲氧基苯甲醛、2-羟基-3-甲氧基苯甲醛和4-溴苯甲酸甲酯为原料，通过Ullmann反应、醛基还原、磷盐生成、Wittig反应、分子内Wittig反应、酚羟基与醛基的保护和脱保护以及烯烃的催化氢化反应等方法完成了一种未见报道的新型双联苄衍生物 (17) 的全合成。所得化合物的结构通过MS、¹H NMR进行确证。MTT法测试目标化合物 17 对U20S细胞和YFP细胞体外抗肿瘤活性，结果显示，目标化合物17的活性强于地钱素C。
- 双联苄衍生物 /
- Ullmann反应 /
- Wittig反应 /
- 合成 /
- 抗肿瘤活性
Abstract: An novel bisbibenzyl derivative was totally synthesized from 3, 4-dimethoxy-6-bromobenzaldehyde, 3-hydroxy-4-methoxybenzaldehyde, 2-hydroxy-3-methoxybenzaldehyde and 4-bromobenzoic acid methyl ester, throuth Ullmann reaction, aldehyde group reduction, phosphorus salt formation, Wittig reaction, intramolecular Wittig reaction, phenolic hydroxy and aldehyde group protection and deprotection as well as catalytic hydrogenation of alkene reaction. The structures of the compounds were confirmed by MS and ¹H NMR. The effects of the target compounds on the proliferation of U2OS cells and YFP cells were evaluated in vitro by MTT assay using marchantin C as the positive control, and the results showed stronger activity of the target product than that of the marchantin C.
- bisbibenzyl derivative /
- Ullmann reaction /
- Wittig reaction /
- synthesis /
- antitumor activity

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参考文献(11)

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一种新型双联苄衍生物的合成及抗肿瘤活性

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出版历程

Synthesis and antitumor activity of a novel bisbibenzyl derivative

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出版历程

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