Abstract: A series of novel compounds bearing imidazo [2, 1-b] thiazole scaffolds were designed and synthesized based on the optimization of the virtual screening hit compound N-(6-morpholinopyridin-3-yl)-2-(6-phenylimidazo [2, 1-b] thiazol-3-yl) acetamide (5a), and tested for their cytotoxicity against human cancer cell lines, including HepG2 and MDA-MB- 231. The results indicated that the compound 2-(6-(4-chlorophenyl) imidazo [2, 1-b] thiazol ...