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目的设计合成一系列4-苯基-2-氨基嘧啶类新型化合物,并测定其对前列腺癌细胞(PC-3)的生长抑制活性。方法以硝基苯乙酮为起始原料,通过嘧啶环合、酰胺缩合、硝基还原、氨基保护及脱保护反应合成目标化合物。采用MTT法测试化合物对前列腺癌PC-3细胞的生长抑制活性;采用均相时间分辨荧光法测定化合物对激酶AKT1的抑制活性。结果与结论合成了9个未见文献报道的4-苯基-2-氨基嘧啶类化合物,其结构经1H-NMR、MS谱确证。化合物9a-1、9a-3、9b-1(5μmol·L-1)对激酶AKT1的抑制率大于60%。
Aim To design and synthesize a series of novel 4-phenyl-2-aminopyrimidine compounds and determine their inhibitory activities on the growth of prostate cancer cells (PC-3). Methods Nitroacetophenone was used as the starting material to synthesize target compounds by pyrimidine cyclization, amide condensation, nitro reduction, amino protection and deprotection. The inhibitory activity of the compounds on the growth inhibition of prostate cancer PC-3 cells was tested by MTT assay. The inhibitory activity of the compounds on AKT1 kinase was determined by the homogeneous time-resolved fluorescence method. RESULTS AND CONCLUSION Nine 9-phenyl-2-aminopyrimidines were synthesized and their structures were confirmed by 1H-NMR and MS. The inhibitory rates of 9a-1, 9a-3, 9b-1 (5μmol·L-1) to AKT1 were more than 60%.