Institution: | a Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine (Ministry of Education), Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China;b Beijing Union Pharmaceutical Factory, Beijing 102600, China |
Abstract: | A series of heterocycle-substituted phthalimide derivatives were synthesized. Structurally diverse derivatives with heterocyclic rings, including furan, imidazo1, 2-a]pyridine, 1, 3, 4-thiadiazine, imidazo2, 1-b]1, 3, 4]thiadiazine, pyrazole, 1, 2, 4-triazolo3, 4-b]1, 3, 4]thiadiazine, thiazole and thiazoline, were obtained by the reactions of α-bromoketone intermediate with various nucleophiles containing oxygen, nitrogen and sulfur atom. Their cytotoxic activity was also evaluated against five human cancer cell lines in vitro. |