Abstract A new class of imidazo [2, 1-b] thiazole chalcone derivatives were synthesized and evaluated for their anticancer activity. These chalcone derivatives show promising activity, with log GI 50 values ranging from− 7.51 to− 4.00. The detailed biological aspects of these derivatives toward the MCF-7 cell line were studied. Interestingly, these chalcone derivatives induced G 0/G 1-phase cell-cycle arrest, down-regulation of G 1-phase cell-cycle ...