Syntheses and antiproliferative evaluation of oxyphenisatin derivatives

Syntheses and structure–antiproliferative relationship for oxyphenisatin analogues are described. The cell proliferation data showed that the presence of substituents (especially F, Cl, Me, CF3, and OMe) in the 6- and 7-position of oxyphenisatin markedly enhanced the potency in the MDA-468 cell line without affecting the MDA-231 cell line. The best compounds from this series showed low nanomolar antiproliferative activity towards the MDA-468 cell line and a 1000-fold selectivity over the MDA-231 cell line.

Graphical abstractThe syntheses and structure–antiproliferative relationship for oxyphenisatin analogues are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide