B环三氟甲基取代的白杨素衍生物合成及其抗癌活性

Synthesis and Anticancer Activities of B-Ring Trifluoromethylated Chrysin Derivatives

目的研究B环三氟甲基取代白杨素衍生物的体外抗癌活性。方法合成B环三氟甲基取代的白杨素衍生物,并通过MTT法检测其对人急性粒细胞性白血病(HL-60)细胞、人结肠癌(HT-29)细胞和人胃癌(SGC-7901)细胞增殖的抑制作用。结果合成了3个三氟甲基B环取代白杨素衍生物,其中化合物6对HL-60、HT-29细胞增殖的抑制作用最强。结论化合物6(7-羟基-4'-三氟甲基-黄酮)具有良好的抗癌活性。

Objective To study the anticancer activity of B - ring trifluoromethylated chrysin derivatives. Methods B - ring trifluoromethylated chrysin derivatives were prepared and their anticancer activities in vitro were evaluated by the standard MTT method. Results Compound 6 showed the strongest activity against HL -60 and HT -29 cells. Conclusion Compound 6 （ 7 - hydroxyl - 4′- trifluoromethyl - flavone ） possessed the potent anticancer activity.