A series of chalcone derivatives bearing benzamide or benzenesulfonamide moieties were synthesized and evaluated for their anti-tumor effect on HCT116, MCF7 and 143B cell lines in vitro. SAR analysis showed that compounds bearing a benzenesulfonamide group had greater potency than those bearing a benzamide group. It was also shown that compounds with a mono-methyl or mono-halogen group at the 3-position on the terminal phenyl ring were more effective than those with trifluoromethyl or methoxy groups. Compound 8e exhibited the most potent anti-tumor activities against HCT116, MCF7 and 143B cell lines, with IC₅₀ values of 0.597, 0.886 and 0.791 μM, respectively. Molecular docking studies and enzymatic assays demonstrated that the anti-tumor activity of compound 8e might be regulated by Cat L and Cat K.

合成了一系列带有苯甲酰胺或苯磺酰胺部分的查耳酮衍生物，并评价了它们对HCT116，MCF7和143B细胞系的体外抗肿瘤作用。SAR分析表明，带有苯磺酰胺基团的化合物比带有苯甲酰胺基团的化合物具有更高的效价。还显示在末端苯环的3-位具有单甲基或单卤素基团的化合物比具有三氟甲基或甲氧基的化合物更有效。化合物8e对HCT116，MCF7和143B细胞系表现出最强的抗肿瘤活性，IC ₅₀值分别为0.597、0.886和0.791μM。分子对接研究和酶促测定表明，化合物8e的抗肿瘤活性可能受Cat L和Cat K调控。