【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。4a R1=H,R2=F,R3=OCH3,R4=H,R5=H4b R1=F,R2=H,R3=OCH3,R4=H,R5=H4c R1=H,R2=H,R3=CF3,R4=H,R5=H4d R1=H,R2=H,R3=OCF3,R4=H,R5=H4e R1=H,R2=F,R3=H,R4=F,R5=H4f R1=H,R2=CF3,R3=H,R4=CF3,R5=H更多还原

【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.4a R1=H,R2=F,R3=OCH3,R4=H,R5=H4b R1=F,R2=H,R3=OCH3,R4=H,R5=H4c R1=H,R2=H,R3=CF3,R4=H,R5=H4d R1=H,R2=H,R3=OCF3,R4=H,R5=H4e R1=H,R2=F,R3=H,R4=F,R5=H4f R1=H,R2=CF3,R3=H,R4=CF3,R5=H更多还原