The antiproliferative and pro-apoptotic effects of 3-deoxy-3α-fluoro-chenodeoxycholic acid and 12β-methyl-3,7-dioxo-17-epi-25-homo-18-nor-5β-cholan-25-oic acid on human breast cancer cell lines. (PubMed, Bioorg Med Chem Lett) - Sep 20, 2026 - "The anti-proliferative activities of nine synthesised derivatives, as well as bardoxolone methyl (CDDO-Me) which is a well-characterised IκB kinase (IKK) and NF-κB inhibitor and Nrf2 activator, were assessed in vitro against two clinically relevant breast cancer cell lines: MCF-7 (estrogen receptor-positive) and MDA-MB-231 (triple negative)...We further discuss structure-activity relationships for these compounds and show that they cause cell death in both cell lines via a statistically significant induction of apoptosis. In addition, in silico assessment predicted appropriate ADMET properties and compliance with Lipinski's rule of five."
Journal • Preclinical • Breast Cancer • Estrogen Receptor Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • ER
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Alex Weymouth-Wilson; Andreas Luxenburger; Bruno Linclau; Divyashree Ravishankar; Francesca Greco; Helen M I Osborn; Joseph M Watts; Lawrence D Harris; Richard H Furneaux; Thibaut Dispa; Wanting Jiao
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