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Bioorg Med Chem Lett. 2012 Jul 1;22(13):4307-9. doi: 10.1016/j.bmcl.2012.05.018. Epub 2012 May 11.

Syntheses and biological activities of sulfoximine-based acyclic triaryl olefins.

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1
Institute of Organic Chemistry, RWTH Aachen University, Landoltweg 1, D-52056 Aachen, Germany.

Abstract

Sulfoximine-based acyclic triaryl olefins 8 and 9 have been prepared and initial studies have been performed to determine their biological profiles. In contrast to their sulfonyl-substituted analog 2 sulfoximines 8 and 9 show low COX inhibitory activity. All compounds affect the estrogen receptors. While sulfone 2 interacts exclusively with ER β, sulfoximines 8 and 9 reveal almost equal blocking potencies for both estrogen receptors, ER α and ER β. In the tested series, triaryl olefin 9a shows the highest inhibitory activities with 91% and 80%, respectively (at 10 μM).

PMID:
22652053
DOI:
10.1016/j.bmcl.2012.05.018
[Indexed for MEDLINE]
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