Synthesis, discovery and preliminary SAR study of benzofuran derivatives as angiogenesis inhibitors

A series of benzofuran derivatives were synthesized and evaluated against HUVEC proliferation. Among these compounds, compound 32 exhibited good inhibitory activity and remarkable selectivity to HUVEC. Our current data suggested that array order of methyl, acrylate and carboxylate groups in benzofuran scaffold is the basic requirement for inhibitory activity against HUVEC proliferation. These results demonstrated that benzofuran scaffold represents a promising structural core to discover a new class of active and selective angiogenesis inhibitors.

Graphical abstractCompound 32 with benzofuran core exhibited good inhibitory activity (IC50 = 4.3 μM) and remarkable selectivity against HUVEC proliferation.Figure optionsDownload full-size imageDownload as PowerPoint slide