丹皮酚查尔酮衍生物的合成及抗肿瘤活性

Synthesis and Anticancer Activity ofPaeonol Chalcones Derivatives

以丹皮酚为原料,与不同取代的苯甲醛经Claisen-Schmidt缩合反应得到3个丹皮酚查尔酮衍生物.目标化合物的结构经过红外光谱、核磁共振氢谱和质谱确证.用MTT法评价了目标化合物对人肝癌HepG2细胞增殖的影响,结果显示,所合成的目标化合物(IC_(50)=7.22~17.41μM)均具有一定的抗肿瘤活性,其中化合物3a(IC_(50)=8.76μM)和3b(IC_(50)=7.22μM)的抗增值活性强于阳性对照药氟尿嘧啶(5-FU,IC_(50)=16.20μM).

Three target compounds from paeonol and different substituted benzaldehyde were synthesized by Claisen-Schmidt reaction and their chemical structures were confirmed by 1H NMR,IR,and MS spectra.All target compounds were evaluated for anti-proliferative activity against HepG2 cells in vitro by thiazolyl blue(MTT)colorimetry method.The results indicated that all target compounds had potent anti-proliferative activity with IC_(50) values of 8.76~17.41μM and compound 3a(IC_(50):8.76μM)was even stronger than 5-Fluorouracil(5-FU)(IC_(50):16.20μM).