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Communication | Special issue | Vol 86, No. 1, 2012, pp.165-170
Published online, 14th August, 2012
DOI: 10.3987/COM-12-S(N)56
FACILE SYNTHESIS AND ESTROGENIC ACTIVITY OF ARYLPYRROLE-BASED BISPHENOL DERIVATIVES

Kiminori Ohta, Fumi Taguchi, and Yasuyuki Endo*

*Faculty of Pharmaceutical Sciences, Tohoku Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai 981-8558, Japan

Abstract

Novel estrogen candidates 6a and 6b incorporating arylpyrrole bisphenol structure were efficiently synthesized in three steps from commercially available materials by means of McMurry coupling and an unexpected BBr3-mediated aromatization. These compounds showed ERα-binding affinity in competitive binding assay and estrogenic activity in MCF-7 cell proliferation assay.