A series of new imidazo[1,2-a]pyridine linked with thiazole/thiophene motif through a keto spacer were synthesized and tested for their cytotoxic potential against three human cancer cell lines including A549, HeLa and U87-MG using MTT assay. Compounds A2, A3, A4, C1 and C2 showed cytotoxicity against all the three cell lines. The selectivity index for compound A4 for A549 and HeLa cells was comparable to that of doxorubicin. Among the synthesized compounds, B5 showed the maximum inhibition of NF-κB activity as ascertained by NF-κB reporter assay (IC₅₀ = 6.5 ± 0.6 µM). Treatment of NCI-H23 cells (EGFR overexpressed, KRAS G12V mutant) with erlotinib and gefitinib along with compounds A4 and B5 indicated synergistic and additive potential of combination therapy.

合成了一系列新的通过酮间隔基与噻唑/噻吩基团连接的咪唑并[1,2- a ]吡啶，并使用MTT法测试了它们对三种人类癌细胞系（包括A549，HeLa和U87-MG）的细胞毒性潜力。化合物A2，A3，A4，C1和C2对所有三种细胞系均显示出细胞毒性。化合物A4对A549和HeLa细胞的选择性指数与阿霉素相当。在合成的化合物中，B5表现出对NF-κB活性的最大抑制作用，这是通过NF-κB报告基因分析确定的（IC ₅₀ = 6.5±0.6 µM）。用埃洛替尼和吉非替尼以及化合物A4和B5处理NCI-H23细胞（EGFR过表达，KRAS G12V突变体）表明联合治疗具有协同作用和加成作用。