2、C3、C23、C28衍生物,并對其體外抗腫瘤活性進(jìn)行研究.方法 以天然產(chǎn)物積雪草酸為先導(dǎo)化合物,對C2、C3、C23位羥基及C28位羧基進(jìn)行結(jié)構(gòu)改造,并采用SRB法對目標(biāo)化合物進(jìn)行初步的體外抗腫瘤活性研究.結(jié)果 設(shè)計(jì)并合成了目標(biāo)化合物,利用MS及1H-NMR確證了結(jié)構(gòu);體外實(shí)驗(yàn)中,積雪草酸衍生物的抗腫瘤活性明顯高于積雪草酸,并優(yōu)于對照藥吉非替尼.結(jié)論 積雪草酸衍生物具有良好的抗腫瘤活性,值得進(jìn)一步研究.;Objective To design and synthesize asiatic acid C2, C3, C23, and C28 derivatives, and to study their antitumor activities in vitro. Methods Asiatic acid was used as starting material to synthesize the target compounds by structural modification at C2, C3, and C23 hydroxyl groups, and C28 carboxyl group. The antitumor activities of the compounds were tested by SRB assay. Results The target compounds were synthesized and characterized by MS and 1H- NMR. The in vitro antitumor activity experiments showed that the antitumor activity of asiatic acid derivatives were higher than those of asiatic acid in vitro, and were better than control drug gefitinib. Conclusion Asiatic acid derivatives have good antitumor activities which could be a valuable candidate for further development."/>

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首頁 > 過刊瀏覽>2015年第30卷第4期 >2015,30(4):355-361. DOI:10.7501/j.issn.1674-5515.2015.04.002
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積雪草酸C2、C3、C23、C28衍生物的合成及其體外抗腫瘤活性研究

Synthesis of asiatic acid C2, C3, C23, and C28 derivatives and their antitumor activities in vitro

發(fā)布日期：2015-04-23
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    [關(guān)鍵詞]
    [摘要]
    目的 設(shè)計(jì)并合成積雪草酸C2、C3、C23、C28衍生物,并對其體外抗腫瘤活性進(jìn)行研究.方法 以天然產(chǎn)物積雪草酸為先導(dǎo)化合物,對C2、C3、C23位羥基及C28位羧基進(jìn)行結(jié)構(gòu)改造,并采用SRB法對目標(biāo)化合物進(jìn)行初步的體外抗腫瘤活性研究.結(jié)果 設(shè)計(jì)并合成了目標(biāo)化合物,利用MS及1H-NMR確證了結(jié)構(gòu);體外實(shí)驗(yàn)中,積雪草酸衍生物的抗腫瘤活性明顯高于積雪草酸,并優(yōu)于對照藥吉非替尼.結(jié)論 積雪草酸衍生物具有良好的抗腫瘤活性,值得進(jìn)一步研究.
    [Key word]
    [Abstract]
    Objective To design and synthesize asiatic acid C2, C3, C23, and C28 derivatives, and to study their antitumor activities in vitro. Methods Asiatic acid was used as starting material to synthesize the target compounds by structural modification at C2, C3, and C23 hydroxyl groups, and C28 carboxyl group. The antitumor activities of the compounds were tested by SRB assay. Results The target compounds were synthesized and characterized by MS and 1H- NMR. The in vitro antitumor activity experiments showed that the antitumor activity of asiatic acid derivatives were higher than those of asiatic acid in vitro, and were better than control drug gefitinib. Conclusion Asiatic acid derivatives have good antitumor activities which could be a valuable candidate for further development.
    [中圖分類號]
    [基金項(xiàng)目]
    國家自然科學(xué)基金資助項(xiàng)目(21372156);遼寧省教育廳高等學(xué)校優(yōu)秀人才支持計(jì)劃資助項(xiàng)目(LR2013017);沈陽市科技計(jì)劃資助項(xiàng)目(F13-316-1-47)