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Synthesis and antiproliferative activity of benzofuran-based analogs of cercosporamide against non-small cell lung cancer cell lines
Ist Teil von
European journal of medicinal chemistry, 2013-11, Vol.69, p.823-832
Ort / Verlag
France: Elsevier Masson SAS
Erscheinungsjahr
2013
Link zum Volltext
Quelle
MEDLINE
Beschreibungen/Notizen
A novel series of 3-methyl-1-benzofuran derivatives were synthesized and screened in vitro for their antiproliferative activity against two human NSCLC cell lines (NSCLC-N6 mutant p53 and A549 wild type p53). Most promising compounds presented a structural analogy with the west part of cercosporamide, a natural product of biological interest. In particular, compounds 10, 12 and 31 showed cytotoxic activities at micromolar concentrations (IC50 < 9.3 μM) and compounds 13, 18 and 32 displayed moderate IC50 values (25–40 μM).
[Display omitted] The access to 3-methyl-1-benzofurans derived from cercosporamide and the corresponding antiproliferative activity against NSCLC cell lines are described.
•3-Methyl-1-benzofurans derived from cercosporamide were synthesized.•Antiproliferative activity against human NSCLC cell lines was investigated.•Some 3-methyl-1-benzofuran-7-carboxamide derivatives exhibited cytotoxic activities.