1. Synthesis and biological evaluation of novel imidazopyrimidin-3-amines as anticancer agents.
- Author
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Mahdavi, Mohammad, Dianat, Shima, Khavari, Behnaz, Moghimi, Setareh, Abdollahi, Mohammad, Safavi, Maliheh, Mouradzadegun, Arash, Kabudanian Ardestani, Sussan, Sabourian, Reyhaneh, Emami, Saeed, Akbarzadeh, Tahmineh, Shafiee, Abbas, and Foroumadi, Alireza
- Subjects
ANTINEOPLASTIC agents ,AMINES ,APOPTOSIS ,IMIDAZOPYRIDINES ,ISOCYANIDES ,CELL lines ,ACRIDINE orange ,ETHIDIUM - 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 IC
50 values of 6.72-14.36 μ m 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. [ABSTRACT FROM AUTHOR]- Published
- 2017
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