Synthesis of novel benzofurocoumarin analogues and their anti-proliferative effect on human cancer cell lines

The synthesis of five new tetracyclic benzofurocoumarin (benzopsoralen) analogues is described. Their inhibitory effects on the growth of three human tumor cell lines (MDA MB 231 (breast adenocarcinoma), HeLa (cervix adenocarcinoma) and TCC-SUP (bladder transitional cell carcinoma) were evaluated, and discussed in terms of structure–activity relationship.

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► Five new benzofurocoumarins were synthesized and their biological activity tested.
► All inhibited significantly the proliferation of three human tumor cell lines.
► Molecular docking and computational studies were carried out.
► Anti-proliferative effect appears to be mainly linked with the inhibition of CYP2A6.