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含氟白藜芦醇衍生物的合成及抗癌活性研究
Synthesis and Anti-cancer of Fluorinated Resveratrol Derivatives
【作者】 姚旭; 刘运美; 曹轩; 罗星; 郑自通; 王小平; 朱炳阳; 郑兴; 廖端芳;
【Author】 Xu YAO,Yun-mei LIU,Xuan CAO,Xing LUO,Zi-tong ZHENG,Xiao-ping WANG,Xing ZHENG,Duan-fang LIAO (The Institute of Pharmacy & Pharmacology,University of South China,Hengyang 421001,China)
【机构】 南华大学药物药理研究所;
【摘要】 白藜芦醇(Resveratrol)是一种天然的抗氧化剂,具有防治心血管疾病,保肝、利肝,抗炎及预防癌症的发生及发展等作用,其中最瞩目的是其在抗肿瘤方面的作用。为了获得高效、低毒的新型先导化合物,我们将能明显增加有机物亲脂性的氟原子引入,利用Wittig-Horner反应设计并合成了一系列含氟白藜芦醇衍生物4a-4f,并通过MTT法检测了这些衍生物对体外培养人结肠癌(HT-29)细胞、人胃癌(SGC-7901)细胞和人急性粒细胞白血病(HL-60)细胞的抑制增殖作用。
【Abstract】 Resveratrol, a phytoalexin found in grapes and other food products, has been demonstrated to be a green anticancer drug. It is know that the introduction of Fluorine into organic molecules often changes their physiological, physical and chemical properties dramatically. To searching for anti-tumor substances with high efficacy, low toxicity and minimum of side effects, we designed and synthesized the target products 4a-4f, and the derivatives were tested for their in vitro anticancer activities against leucocythemia (HL-60), colorectal adenocarcinoma (HT-29) and human gastric adenocarcinoma (SGC-7901) cell lines by MTT-Based Assay.
- 【会议录名称】 2010年中国药学大会暨第十届中国药师周论文集
- 【会议名称】2010年中国药学大会暨第十届中国药师周
- 【会议时间】2010-11
- 【会议地点】中国天津
- 【分类号】R284.1;R285
- 【主办单位】中国药学会(Chinese Pharmaceutical Association)、天津市人民政府