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

• 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.

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).

The access to 3-methyl-1-benzofurans derived from cercosporamide and the corresponding antiproliferative activity against NSCLC cell lines are described.Figure optionsDownload as PowerPoint slide