Estrone 3-methyl ether is a synthetic estrogen and derivative of estrone .1 It stimulates proliferation of estrogen-dependent MCF-7 breast cancer cells in vitro when used at concentrations ranging from 0.16 to 20 μM but lacks estrogen receptor (ER) binding activity (IC50s = >100 μM for ERα and ERβ). Estrone 3-methyl ether has been used in the synthesis of various estrogen receptor modulators.2
References
1. Alsayari, A., Kopel, L., Ahmed, M.S., et al. Design, synthesis, and biological evaluation of steroidal analogs as estrogenic/anti-estrogenic agents. Steroids 118, 32-40 (2017).
2. Kuznetsov, Y.V., Levina, I.S., Scherbakov, A.M., et al. New estrogen receptor antagonists. 3,20-Dihydroxy-19-norpregna-1,3,5(10)-trienes: Synthesis, molecular modeling, and biological evaluation. Eur. J. Med. Chem. 143, 670-682 (2018).