Synthesis of hybrid acetogenins, α,β-unsaturated-γ-lactone-free nitrogen-containing heterocyclic analogues, and their cytotoxicity against human cancer cell lines

A series of α,β-unsaturated-γ-lactone-free nitrogen-containing heterocyclic analogues of solamin, a natural mono-THF acetogenin, have been synthesized and their cytotoxicity was investigated against 39 tumor cell lines. One of them, 1-methylpyrazol-5-yl derivative, showed selective increase of cytotoxicity against NCI-H23 with 80 times higher potency than solamin.

Graphical abstractA series of nitrogen-containing heterocyclic analogues of solamin, a natural mono-THF acetogenin, have been synthesized and investigated for their cytotoxicity against 39 tumor cell lines.Figure optionsDownload full-size imageDownload as PowerPoint slide