目标：采用基于片段的设计和合成方法，实施构建三个新的氨基吡啶酮连接苯并咪唑衍生物系列，作为潜在的抗癌候选药物，并具有显著的CDK9抑制作用。材料和方法：所有合成的化合物均提交至国家癌症研究所60个细胞系和七剂量细胞毒性测试对三个癌细胞。结果：化合物2、4a、4c、4d、6a和8a表现出显著的细胞毒性和选择性，IC50范围为7.61-57.75 μM。无论是体外还是体内，4a、6a和8a在机理上显示出强效的CDK9抑制作用，IC50值为0.424-8.461 μM。化合物6a能够使细胞周期在S期停滞并在MCF-7细胞中诱导细胞凋亡。结论：化合物6a是一种有希望的CDK9抑制剂，值得进一步研究作为抗癌治疗药物。

Aim: A fragment-based design and synthesis of three novel series of aminopyridone-linked benzimidazoles as potential anticancer candidates with significant CDK9 inhibition was implemented. Materials & methods: All synthesized compounds were submitted to National Cancer Institute 60 cell lines and seven-dose cytotoxicity toward three cancer cells. Results: Compounds 2, 4a, 4c, 4d, 6a and 8a exhibited significant cytotoxicity and selectivity with IC50 range of 7.61-57.75 μM. Regarding the mechanism either in vitro or in silico, 4a, 6a and 8a displayed potent CDK9 inhibition with IC50 value of 0.424-8.461 μM. Compound 6a arrested the cell cycle at S phase and induced apoptosis in MCF-7 cells. Conclusion: Compound 6a is a promising CDK9 inhibitor that warrants additional research for cancer treatment.