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以2-氰基乙酰胺为起始原料,与三乙氧基取代化合物经加成反应制得取代烯酰胺类化合物(3a~3c);3a~3c与芳肼经环合反应得取代吡唑-4-甲酰胺类化合物(5a~5d);5a~5d与酰氯经酰化反应合成了6个新型的1-芳基-3-取代-5-取代氨基-4-吡唑甲酰胺类化合物(7a~7f),其结构经1H NMR,MS和元素分析表征。抗肿瘤活性测试结果表明,7a~7f对人乳腺癌细胞(A)、人宫颈癌细胞(B)和人肝癌细胞(C)有一定抑制作用,其中3-甲基-5-[4-(甲磺酰胺基)苯甲酰胺]-1-苯基-1H-吡唑-4-甲酰胺(7f)的抑制活性最好,对A,B和C的IC50分别为3.25μM,8.74μM和10.47μM。
The substituted enamide compounds (3a ~ 3c) were prepared by the reaction of 2-cyanoacetamide with triethoxy substituted compounds. The substituted pyrazoles were obtained by cyclization reaction of 3a ~ 3c with arylhydrazine 4-carboxamides (5a ~ 5d). Six novel 1-aryl-3-substituted-5-substituted amino-4-pyrazolecarboxamides (7a ~ 7f). Its structure was characterized by 1H NMR, MS and elemental analysis. The results of antitumor activity test showed that 7a ~ 7f could inhibit human breast cancer cells (A), human cervical cancer cells (B) and human hepatocellular carcinoma cells (C), and 3-methyl-5- [4- Methanesulfonamido) benzamide] -1 -phenyl- 1 H-pyrazole-4-carboxamide (7f) with the IC50 of 3.25 μΜ, 8.74 μΜ and 10.47 for A, B and C, respectively μM.