4-oxo-27-TBDMS Withaferin A

Description

4-oxo-27-TBDMS Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.¹ It is cytotoxic to A2780 ovarian cancer cells (IC₅₀ = 17 μM) but not to carboplatin-resistant A2780 (A2780/CP70) cells (IC₅₀ = >100 μM). It is selective for A2780 cells over non-cancerous ARPE19 cells (IC₅₀ = 1,660 μM). 4-oxo-27-TBDMS Withaferin A induces DNA fragmentation in A2780 cells.

References

1. Perestelo, N.R., Llanos, G.G., Reyes, C.P., et al. Expanding the chemical space of withaferin A by incorporating silicon to improve its clinical potential on human ovarian carcinoma cells J. Med. Chem. 62(9),4571-4585(2019).