Figure 2. OBHS-N analogs exhibit growth-inhibitory and anti-inflammatory effects.
(a) MCF-7, MDA-MB231 and OVCAR3 cells were cultured in steroid free media, treated on days 1 and 4 with 10 μM OBHS-N compounds, and analyzed on day 7. Ligands were grouped by R2 group. Each data point represents the average (mean) number of cells observed in triplicate experiments with a distinct compound, and is shown as a percentage of vehicle-treated cells. Dotted lines represent values for 10 nM estradiol (E2, black), 1 μM 4-OHT (cyan) and 1 μM fulvestrant (Fulv, red).
(b) Dose-dependent suppression of ERα+ breast cancer cell proliferation by tamoxifen, fulvestrant or compound 12. MCF-7 or ZR-75 cells were treated as in panel a, with increasing doses of ligands. Data represents mean ± s.e.m of triplicate values.
(c) Steroid-deprived MCF-7 cells were treated with vehicle, 10 ng/ml TNFα, or TNFα + OBHS-N compounds, E2, 4-OHT or fulvestrant (Fulv) at 10 μM for 24 hr. Media was collected and IL-6 protein levels were measured by AlphaLISA. Each point represents average of n = 3.