| Institution: | 1. Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran;2. Department of Chemistry, Faculty of Sciences, Shahid Chamran University, Ahvaz, Iran;3. Institute of Biochemistry and Biophysics, Department of Biochemistry, University of Tehran, Tehran, Iran;4. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran;5. Department of Toxicology and Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran;6. Department of Biotechnology, Iranian Research Organization for Science and Technology, Tehran, Iran;7. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran;8. Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran |
| Abstract: | Groebke–Blackburn–Bienayme reaction has been utilized for the synthesis of new imidazo1,2‐a]pyrimidine derivatives as novel anticancer agents. The cytotoxic activities of compounds were evaluated against human cancer cell lines including MCF‐7, T‐47D, and MDA‐MB‐231, compared with etoposide as the standard drug. Among the tested compounds, hydroxy‐ and/or methoxy‐phenyl derivatives ( 6a–c and 6k ) with IC50 values of 6.72–14.36 μm were more potent than etoposide against all cell lines. The acridine orange/ethidium bromide double staining and DNA fragmentation studies demonstrated that the cytotoxic effect of 3‐hydroxy‐4‐methoxyphenyl derivative 6c is associated with apoptosis in cancer cells. |
