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

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Chen XY, Park SJ, Buschmann H, De Rosa M, Bolm C

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

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

PubMed ID
22652053 [ View in PubMed
]
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 beta, sulfoximines 8 and 9 reveal almost equal blocking potencies for both estrogen receptors, ER alpha and ER beta. In the tested series, triaryl olefin 9a shows the highest inhibitory activities with 91% and 80%, respectively (at 10 muM).

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DiethylstilbestrolEstrogen receptor alphaIC 50 (nM)770N/AN/ADetails
DiethylstilbestrolEstrogen receptor betaIC 50 (nM)610N/AN/ADetails
IndomethacinProstaglandin G/H synthase 1IC 50 (nM)44N/AN/ADetails
RofecoxibProstaglandin G/H synthase 2IC 50 (nM)170N/AN/ADetails