In order to discover new anticancer drug leads, a series of novel alkylamino pyrimidine derivatives were designed and synthesized based on our previous work via a ring-opening strategy. Biological evaluation with four human cancer cell lines (MDA-MB-231, A549, HepG2, and MCF-7) showed that most of these compounds possessed moderate to potent antiproliferative activities. The most promising compound 7w displayed a three-fold improvement compared with commercial anticancer drug fluorouracil in inhibiting HepG2 cell proliferation with IC₅₀ value of 10.37 μM. Moreover, flow-activated cell sorting analysis suggested that compound 7w mainly arrested HepG2 cells in G₂/M stage. Hence, it could serve as a promising lead for the design of novel anticancer small-molecule drugs.

为了发现新的抗癌药物，根据我们以前的工作，通过开环策略设计并合成了一系列新型的烷基氨基嘧啶衍生物。用四种人类癌细胞系（MDA-MB-231，A549，HepG2和MCF-7）进行生物学评估，结果表明，这些化合物大多数都具有中等至有效的抗增殖活性。与商用抗癌药物氟尿嘧啶相比，最有希望的化合物7w在抑制HepG2细胞增殖方面显示出三倍的改善，IC ₅₀值为10.37μM。此外，流激活细胞分选分析表明，化合物7w主要在G _2中阻滞了HepG2细胞。/ M阶段。因此，它可以作为新型抗癌小分子药物设计的有前途的线索。