Synthesis and antitumor activity of 5,6-dihydro-17-hydroxy icogenin analogs

Four 5,6-dihydro-17-hydroxy icogenin analogs were designed and synthesized. Their in vitro antitumor activities were tested by the standard MTT assay. Compound 22 (IC50 = 3.38–8.30 μM) and compound 23 (IC50 = 1.90–9.69 μM) showed potential antitumor activities against the entire tested seven cancer cell lines. The SAR (structure activity relationship) research showed that the introduction of 17-hydroxy lowered the antitumor activity to an extent.

Graphical AbstractFour 5,6-dihydro-17-hydroxy icogenin analogs were synthesized and tested for antitumor activity.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► We designed and synthesized four 5,6-dihydro-17-hydroxy icogenin analogs. ► 22 (IC50 = 3.38–8.30 μM) and 23 (IC50 = 1.90–9.69 μM) showed potential antitumor activity. ► The introduction of 17-hydroxy lowered the antitumor activity to an extent.