Synthesis and biological evaluation of novel imidazopyrimidin-3-amines as anticancer agents.
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.
['Mahdavi|Mohammad|M|', 'Dianat|Shima|S|', 'Khavari|Behnaz|B|', 'Moghimi|Setareh|S|', 'Abdollahi|Mohammad|M|', 'Safavi|Maliheh|M|', 'Mouradzadegun|Arash|A|', 'Kabudanian Ardestani|Sussan|S|', 'Sabourian|Reyhaneh|R|', 'Emami|Saeed|S|', 'Akbarzadeh|Tahmineh|T|', 'Shafiee|Abbas|A|', 'Foroumadi|Alireza|A|']
D000588:Amines D000970:Antineoplastic Agents D045744:Cell Line, Tumor D049109:Cell Proliferation D053938:DNA Fragmentation D006801:Humans D061986:MCF-7 Cells D008856:Microscopy, Fluorescence D011743:Pyrimidines D013329:Structure-Activity Relationship
anticancer agents Groebke-Blackburn-Bienayme reaction apoptosis imidazo[1, 2-a]pyrimidine isocyanide