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Synthesis and biological evaluation of novel imidazopyrimidin-3-amines as anticancer agents. 2017
Mohammad Mahdavi, and
Shima Dianat, and
Behnaz Khavari, and
Setareh Moghimi, and
Mohammad Abdollahi, and
Maliheh Safavi, and
Arash Mouradzadegun, and
Sussan Kabudanian Ardestani, and
Reyhaneh Sabourian, and
Saeed Emami, and
Tahmineh Akbarzadeh, and
Abbas Shafiee, and
Alireza Foroumadi
Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran.
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.
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