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熊果酸衍生物的合成及其抗肿瘤活性评价

Synthesis and antitumor activity evaluation of ursolic acid derivatives.

作者信息

Meng Yan-Qiu, Xu Chuan-Dong, Yu Ting-Ting, Li Wei, Li Qian-Wen, Li Xiao-Xiao

机构信息

Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China.

出版信息

J Asian Nat Prod Res. 2020 Apr;22(4):359-369. doi: 10.1080/10286020.2019.1571488. Epub 2019 Mar 4.

DOI:10.1080/10286020.2019.1571488
PMID:30829054
Abstract

Eighteen uronic acid derivatives were designed and synthesized, and the cytotoxicities of two cancer cell lines (BEL7402 and SGC7901) were evaluated by MTT assay. The results showed that the inhibitory rate of the compounds on both cell lines was significantly higher than the parent compound. The IC of compounds II, II, III, and III are comparable or stronger than the positive control drug, the interactions between compounds II, II, III, III, and NF-κB were also studied by docking simulations.

摘要

设计并合成了18种糖醛酸衍生物,通过MTT法评估了两种癌细胞系(BEL7402和SGC7901)的细胞毒性。结果表明,这些化合物对两种细胞系的抑制率均显著高于母体化合物。化合物II、II、III和III的半数抑制浓度与阳性对照药物相当或更强,还通过对接模拟研究了化合物II、II、III、III与核因子κB之间的相互作用。

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