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. 2013 Nov:69:823-32.
doi: 10.1016/j.ejmech.2013.09.013. Epub 2013 Sep 18.

Synthesis and antiproliferative activity of benzofuran-based analogs of cercosporamide against non-small cell lung cancer cell lines

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Synthesis and antiproliferative activity of benzofuran-based analogs of cercosporamide against non-small cell lung cancer cell lines

Marc-Antoine Bazin et al. Eur J Med Chem. 2013 Nov.

Abstract

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).

Keywords: Antiproliferative activity; Benzofuran; Cercosporamide; NSCLC.

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