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Upstream product

• 4693-91-8 4-methoxyphenyl-acetic chloride 
• 100-66-3 methoxybenzene 
• 21757-13-1 1,2,4-Tris-(p-methoxyphenyl)-1,4-butandion 
• 120-44-5 1,4-di(4-methoxyphenyl)ethanone 
• 1314125-84-2 2,3,5-tris(4-methoxyphenyl)-1-methyl-1H-pyrrole 

Relevant academic research and scientific papers

Development of 2,3,5-triaryl-1H-pyrroles as estrogen receptorα selective ligands

1-Alkyl-2,3,5-triaryl-1H-pyrroles (for which alkyl=methyl, ethyl, n-propyl, or 2-methylpropyl) were tested for stability, estrogen receptor (ER) binding, and inhibition of tumor cell growth. These pyrroles (typeB) showed higher stability in aqueous solution than their 1,2,4-triaryl-1H-pyrrole congeners (typeA pyrroles), exclusive ERα binding (no ERβ interaction), and a hormonal profile of partial agonists at ERα. The most potent compound, 1-(2-methylpropyl)-2,3,5-tris(4-hydroxyphenyl)-1H-pyrrole (5d), was less active than the lead structure 1,3,5-tris(4-hydroxyphenyl)-4-propyl-1H-pyrazole (PPT) in MCF-7 cells stably transfected with the plasmid EREwtcluc (MCF-7/2a), but more potent in U2-OS/α cells. Furthermore, 5d showed weak anti-estrogenic properties (IC50=310nM). An additional propyl chain at C4 decreased the stability and pharmacological effects.