Novel derivatives of diosgenin: design, synthesis and anti-tumor activity

Diosgenin can inhibit the growth of A375 and K562 cell lines and induce their apoptosis with an effect on pro-apoptotic members of Bcl-2 family.  To study the SAR of diosgenin derivatives, and to improve the anti-tumor activity of diosgenin, a series of novel diosgenin derivatives were designed and synthesized.  Their anti-tumor activities in vitro were evaluated.  The results revealed that most of the new derivatives had potent effects against K562, A375 and A549 (three tumor cell lines) in vitro, and had no or less effect against H293 and L02 (two normal cell lines).  Particularly, some compounds (e.g. 1, 6−8) showed excellent activities on K562 with IC₅₀ values ranging from 1.96 to 4.35 μmol·L⁻¹.