C-Ring Oxidized Estrone Acetate Derivatives: Assessment of Antiproliferative Activities and Docking Studies

C-Ring oxidized estrone acetate derivatives as antiproliferative agents were prepared and tested against five cancer cell lines by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Flow cytometry assays to evaluate viability modifications in cycle phases molecular docking research estrogen receptor α, steroid sulfatase, 17β-hydroxysteroid dehydrogenase type 1 performed. 9α-Hydroxy,11β-nitrooxyestrone was most cytotoxic molecule hormone-dependent cells. Furthermore, flow experiments revealed that this 9α-hydroxy,11β-nitrooxy derivative markedly reduced HepaRG cells (~92%) after 24 h of treatment. However, 9α-hydroxyestrone led selective inhibition growth, inducing a G0/G1 arrest, did not originate proliferation effect on T47-D Docking studies estimated generally lower affinity these compounds α than predicted for 17β-estradiol. Therefore, structural modification can be interest develop new anticancer estrane devoid estrogenic action.