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Synthesis and Biological Evaluation of Novel Imidazopyrimidin-3-Amines As Anticancer Agents Publisher Pubmed



Mahdavi M1 ; Dianat S2 ; Khavari B3 ; Moghimi S4 ; Abdollahi M5 ; Safavi M6 ; Mouradzadegun A2 ; Kabudanian Ardestani S3 ; Sabourian R7 ; Emami S8 ; Akbarzadeh T4, 7 ; Shafiee A4 ; Foroumadi A1, 4
Authors

Source: Chemical Biology and Drug Design Published:2017


Abstract

Groebke–Blackburn–Bienayme reaction has been utilized for the synthesis of new imidazo[1,2-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. © 2016 John Wiley & Sons A/S
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