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Synthesis of chrysin derivatives and screening of antitumor activity.
Journal of Asian Natural Products Research ( IF 1.7 ) Pub Date : 2019-03-19 , DOI: 10.1080/10286020.2019.1586677
Ni Chen 1 , Ru Wang 1 , Liu-Jun Lu 1 , Li-Jian Yan 1 , Li-Li Bai 1 , Yan Fu 1 , Ying Wang 1 , De-Qian Peng 1 , Xun Chen 1 , Can-Hong Wang 2 , Juan Li 1 , Ke Zhao 1
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A series of aromatic or long-chain chrysin derivatives (1-10) were synthesized by esterification of chrysin and acyl chloride. The chemical structures of these compounds were determined by mass spectrum (MS), 1H NMR, and 13C NMR spectra. Though aromatic chrysin derivatives (1-9) with a rigid structure were hard to dissolve in common organic solvents, the long-chain chrysin derivative (10) with a flexible structure had better solubility, and its anticancer activity (IC50 = 14.79 μmol/L) against liver cancer cell lines was 5.4 times better than chrysin (IC50 = 74.97 μmol/L), which showed superposition of pharmacological activity.

中文翻译:

菊花素衍生物的合成和抗肿瘤活性的筛选。

一系列的芳香族或长链菊花链衍生物(1-10)是通过对菊花链和酰氯的酯化反应合成的。这些化合物的化学结构由质谱(MS),1 H NMR和13 C NMR光谱确定。尽管具有刚性结构的芳香族菊花衍生物(1-9)难溶于普通有机溶剂,但具有柔性结构的长链菊花衍生物(10)具有更好的溶解性,并且其抗癌活性(IC50 = 14.79μmol/ L) )对肝癌细胞的抵抗力比chrysin高5.4倍(IC50 = 74.97μmol/ L),表现出药理活性的叠加。
更新日期:2020-04-20
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