withaferin a

WITHAFERIN A is a novel class of NFkappaB inhibitors, which hold promise as novel anti-inflammatory agents for treatment of various inflammatory disorders and or cancer.

3-(2-Hydroxyethyl) thio withaferin A, a derivative of Withaferin A, is a steroidal lactone that inhibits NF-kB activation and targets vimentin, showcasing potent anti-inflammatory and anticancer properties. It also acts as an inhibitor of endothelial protein C receptor (EPCR) shedding [1] [2] [3].

3-Ethylthio withaferin A, a derivative of Withaferin A, is a compound known for its inhibitory action on NF-κB (NF-kB).

4,27-Dimethyl withaferin A, a synthetic analog of withanolide natural products, exhibits potential in the study of neurodegenerative diseases[1].

4-Methylwithaferin A, a withaferin A analog, exhibits antitumor activity [1].

4-oxo Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.1 It is cytotoxic to A2780 ovarian cancer cells and carboplatin-resistant A2780 (A2780/CP70) cells (IC50s = 7.3 and <1 μM, respectively) and is 4.4-fold selective for A2780 cells over non-cancerous ARPE19 cells.References1. 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). 4-oxo Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.1 It is cytotoxic to A2780 ovarian cancer cells and carboplatin-resistant A2780 (A2780/CP70) cells (IC50s = 7.3 and <1 μM, respectively) and is 4.4-fold selective for A2780 cells over non-cancerous ARPE19 cells. References1. 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).

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.References1. 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). 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. References1. 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).

4-epi-Withaferin A (compound 28), an analogue of Withaferin A, exhibits enhanced cytotoxicity and cytoprotective heat-shock-inducing activity (HSA), showing promise for investigating protein aggregation-associated diseases by stimulating cellular defense mechanisms [1].

27-O-acetyl-withaferin A is a natural product

27-O-(tert-Butyldimethylsilyl)withaferin A (compound 9a), a natural withanolide known for inducing apoptosis, exhibits antiproliferative effects on HeLa, A-549, and MCF-7 human cancer cell lines, as well as on normal Vero cells [1].