A novel series of 2-(benzo[4,5]imidazo[2,1-b]thiazol-3-yl)acetamide derivatives was synthesized and their antitumor activities against the cancer cell lines HeLa and HepG2, which are abundant and low in the expression of EGFR, respectively, and the human normal cell lines (HL7702 and HUVEC) were evaluated by the MTT colorimetric assay. This evidence concerns the gene EGFR and cancer.