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目的寻找具有抗癌活性的新吡咯并吡嗪酮类化合物。方法以吡咯、对氨基苯乙酮为原料,经Friedel-Crafts酰化、醇解、亲核取代、环合及醇解反应制得母体化合物2-甲基-3-对氨基苯基吡咯并[1,2-a]吡嗪-1(2H)-酮,再通过酰基化/磺酰基化和烷基化反应引入酰基和烷基即制得系列吡咯并吡嗪酮类化合物。结果合成了8个未见文献报道的吡咯并吡嗪酮类化合物,其结构经1H-NMR、MS和IR谱确证。结论8个目标化合物的体外抗乳腺癌细胞、肝癌细胞和肺癌细胞的活性试验结果显示,化合物4、5具有明显的抗癌活性。
Aim To find new pyrrolopyrazinone compounds with anticancer activity. Methods Starting from pyrrole and p-aminoacetophenone, Friedel-Crafts acylation, alcoholysis, nucleophilic substitution, cyclization and alcoholysis gave 2-methyl-3-p- aminophenylpyrrolo [ 1,2-a] pyrazin-1 (2H) -one. A series of pyrrolopyrazinones were prepared by acyl and sulfonylation and alkylation reactions. Results Eight novel pyrrolopyrazinones were synthesized and their structures were confirmed by 1H-NMR, MS and IR. Conclusion The activity test of eight target compounds in vitro against breast cancer cells, liver cancer cells and lung cancer cells showed that compounds 4 and 5 have obvious anticancer activity.