磷脂酰肌醇3-激酶(PI3K)信号通路的不正常表达常与肿瘤发生、进展和恶性预后相关。因此，PI3K抑制剂对癌症的治疗引起了重要兴趣。本研究设计、合成了一系列新型6-(咪唑并[1,2-a]吡啶-6-基)喹唑啉衍生物，并通过1H NMR、13C NMR和HRMS光谱分析进行表征。在体外抗癌测试中，大多数合成化合物对各种肿瘤细胞系表现出亚微摩尔水平的抑制活性，其中13k是最有效的化合物，对所有测试细胞系的IC50值在0.09 μΜ至0.43 μΜ之间。此外，13k通过PI3Kα的抑制剂作用在HCC827细胞中诱导细胞周期阻滞在G2/M期和细胞凋亡，其抑制剂IC50值为1.94 nM。这些结果表明化合物13k可能成为PI3Kα抑制剂开发的前导化合物。

Aberrant expression of the phosphatidylinositol 3-kinase (PI3K) signalling pathway is often associated with tumourigenesis, progression and poor prognosis. Hence, PI3K inhibitors have attracted significant interest for the treatment of cancer. In this study, a series of new 6-(imidazo[1,2-a]pyridin-6-yl)quinazoline derivatives were designed, synthesized and characterized by 1H NMR, 13C NMR and HRMS spectra analyses. In the in vitro anticancer assay, most of the synthetic compounds showed submicromolar inhibitory activity against various tumour cell lines, among which 13k is the most potent compound with IC50 values ranging from 0.09 μΜ to 0.43 μΜ against all the tested cell lines. Moreover, 13k induced cell cycle arrest at G2/M phase and cell apoptosis of HCC827 cells by inhibition of PI3Kα with an IC50 value of 1.94 nM. These results suggested that compound 13k might serve as a lead compound for the development of PI3Kα inhibitor.