Estrogen receptor antagonist 2

What is Estrogen receptor antagonist 2

**Introduction to Estrogen Receptor Antagonist 2** Estrogen Receptor Antagonist 2 is a potent and selective small-molecule inhibitor designed to target and block estrogen receptor (ER) signaling pathways. This compound exhibits high affinity for ERα and ERβ, effectively suppressing estrogen-dependent proliferation in hormone-sensitive cancers, such as breast and ovarian cancer. With its optimized pharmacokinetic profile, Estrogen Receptor Antagonist 2 demonstrates strong therapeutic potential in preclinical studies, offering improved efficacy and reduced off-target effects compared to existing antiestrogens. Its mechanism of action involves competitive binding to estrogen receptors, preventing transcriptional activation and downstream oncogenic signaling. This makes it a promising candidate for further development in endocrine therapy and combination treatments for ER-positive malignancies.

Preparation Process: To prepare **Estrogen Receptor Antagonist 2**, start by dissolving **4-hydroxybenzaldehyde** (1.0 equiv) in dry DMF under nitrogen. Add **K₂CO₃** (2.0 equiv) and **1,2-dibromoethane** (1.2 equiv), then heat at 80°C for 12 h. After cooling, extract with ethyl acetate, wash with water, and dry over Na₂SO₄. Concentrate to obtain the intermediate **4-(2-bromoethoxy)benzaldehyde**. Next, react this intermediate with **4-fluorophenylmagnesium bromide** (1.1 equiv) in THF at 0°C, then quench with NH₄Cl. Oxidize the resulting alcohol with PCC to yield the ketone. Finally, react with **hydroxylamine hydrochloride** (1.5 equiv) in pyridine at reflux to form the oxime, yielding **Estrogen Receptor Antagonist 2**.

Usage Scenarios: Estrogen receptor antagonist 2 is primarily used in research and therapeutic settings to block the activity of estrogen receptors (ER). It is employed in studies investigating hormone-dependent cancers, such as breast and ovarian cancer, where estrogen signaling promotes tumor growth. By inhibiting ER activation, this compound helps suppress cancer cell proliferation. Additionally, it is utilized in endocrine therapy to treat ER-positive malignancies, often in combination with other agents. Researchers also use it to explore estrogen-related pathways in reproductive health, bone metabolism, and cardiovascular function. Its role in modulating estrogenic effects makes it valuable in both clinical and experimental contexts.

Estrogen receptor antagonist 2 Basic Info

Safely Info

Estrogen receptor antagonist 2 Price