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Synthesis and biological evaluation of novel imidazopyrimidin‐3‐amines as anticancer agents
Author(s) -
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,
Foroumadi Alireza
Publication year - 2017
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12904
Subject(s) - acridine orange , ethidium bromide , chemistry , etoposide , cytotoxic t cell , dna fragmentation , apoptosis , pyrimidine , podophyllotoxin , cancer cell , acridine , stereochemistry , cytotoxicity , cell culture , combinatorial chemistry , pharmacology , biochemistry , in vitro , dna , cancer , biology , programmed cell death , organic chemistry , chemotherapy , genetics
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.