New tetrazole fused imidazopyridine derivatives (12a–j) were developed to exploit their cytotoxic activity towards cancer cell lines-MCF7, A549, and MDA-MB-231, utilizing MTT reduction assay with doxorubicin as standard drug. The compounds 12 h and 12j demonstrated strong anticancer activity bearing IC50 values 1.44 μM and 1.33 μM against A549 cell line.