关键词: 射干苷元, 衍生物, MTT法, 人结肠癌细胞株, 人肺癌细胞株, 人肝癌细胞株

Abstract: Five compounds were synthesized with tectorigenin as the lead compound,and the antitumor activity of the compounds in vitro was investigated by comparing with tectorigenin to provide basis for the research and development of new antitumor drugs.In chemical experiments,compounds 1-5 were synthesized by sulfonation,methylation,ethylation,and their structures were determined according to the data of IR,UV,MS and NMR,respectively,which were tectorigenin-5′-sodium sulfonate,4′,7-dimethyl tectorigenin,4′,7-dimethyl tectorigenin-5′-sodium sulfonate,4′,7-diethyl tectorigenin,4′,7-diethyl tectorigenin-5′-sodium sulfonate,respectively,in which compound 5 was proved to be a new compound.The results of activity study showed that the compounds could inhibit the proliferation of HCT116,A549 and HepG2 cells in vitro,and the effects were significantly stronger than the same dose of tectorigenin group,especially compound 3,which had IC₅₀ of 33.67 μM for A549,and compound 5 which had IC₅₀ of 24.71 and 32.42 μM for HCT116 and HepG2,respectively.The anti-tumor activity is obvious,which has a good development and utilization value.

Key words: tectorigenin, derivative, MTT, HCT116, A549, HepG2