A series of novel azacalix[2]arene[2]pyrimidines were synthesized, and evaluated for their antiproliferative activities against A549, MCF7, SH-SY5Y and CNE human cancer cell lines in vitro by using the CCK-8 assay. A number of compounds showed low micromolar antiproliferative activities against MCF7 cell line. Compound 4j, containing a pyrrolidine moiety, exhibited the strongest inhibitory activity with an IC₅₀ value of 0.58 μM. Furthermore, breast cancer cells were used to explore the inhibition mechanism of these azacalix[2]arene[2]pyrimidines. The results suggested these compounds were involved in inducing cell apoptosis via up-regulation of caspase-3 and caspase-9 protein expression, and the cell cycle was arrested at the S phase. Our reports here represent the first studies on the biological activities of azacalix[2]arene[2]pyrimidines.

合成了一系列新颖的氮杂杯[2]芳烃[2]嘧啶，并通过CCK-8测定了其体外对A549，MCF7，SH-SY5Y和CNE人癌细胞系的抗增殖活性。许多化合物对MCF7细胞系表现出低的微摩尔抗增殖活性。含有吡咯烷部分的化合物4j表现出最强的抑制活性，IC ₅₀值为0.58μM。此外，乳腺癌细胞被用来探索这些azacalix [2] arene [2] pyrimidines的抑制机制。结果表明这些化合物参与通过以下途径诱导细胞凋亡caspase-3和caspase-9蛋白表达上调，细胞周期停在S期。我们的报告在这里代表了对azacalix [2] arene [2] pyrimidines的生物学活性的首次研究。