Synthesis of gibberellin derivatives with anti-tumor bioactivities

A series of gibberellin based molecules were designed and synthesized. Gibberellin derivatives bearing two α,β-unsaturated ketone units showed strong anticancer activities in MTT assay towards a number of human cancer cell lines including HT29, A549, HepG2 and MKN28. The most potent gibberellin derivative (compound 10, IC50 = 2.9 μM against HT29) inhibited completely the topoisomerase I activity at 8 μg/mL level.

A series of gibberellin based molecules were designed and synthesized. Gibberellin derivatives bearing two α,β-unsaturated ketone units showed strong anticancer activities in MTT assay towards a number of human cancer cell lines including HT29, A549, HepG2 and MKN28. The most potent gibberellin derivative (R = Me, IC50 = 2.9 μM against HT29) inhibited completely the topoisomerase I activity at 8 μg/mL level.Figure optionsDownload as PowerPoint slide