10'-Desmethoxystreptonigrin is an antibiotic originally isolated from Streptomyces and a derivative of the antibiotic streptonigrin. It is active against a variety of bacteria, including S. aureus, S. faecalis, E. coli, K. pneumoniae, and P. vulgaris (MICs = 0.4, 1.6, 3.1, 3.1 and 0.4 μg/ml, respectively). 10'-Desmethoxystreptonigrin is cytotoxic to HCT116 colon and A2780 ovarian cancer cells (IC50s = 0.004 and 0.001 μg/ml, respectively), as well as HCT116 cells resistant to etoposide and teniposide and cisplatin-resistant A2780cells (IC50s = 0.003, 0.001, and 0.01 μg/ml, respectively). 10'-Desmethoxystreptonigrin is also an inhibitor of p21ras farnesylation (IC50 = 21 nM).
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 A2780cells over non-cancerous ARPE19 cells (IC50 = 1,660 μM). 4-oxo-27-TBDMS Withaferin A induces DNA fragmentation in A2780cells.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 A2780cells over non-cancerous ARPE19 cells (IC50 = 1,660 μM). 4-oxo-27-TBDMS Withaferin A induces DNA fragmentation in A2780cells. 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 A2780cells 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 A2780cells 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).