Sperberweg 15

Aachen, Germany

Sperberweg 15

Aachen, Germany
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Chen X.Y.,RWTH Aachen | Buschmann H.,Sperberweg 15 | Bolm C.,RWTH Aachen
Synlett | Year: 2012

Sulfoximine- and sulfilimine-based diamino-diphenyl sulfone (DAPSON) analogues have been prepared and their COX-1 and COX-2 inhibition potencies as well as LTBand TNF binding properties were studied. Furthermore, their antiproliferative activities on cancer cell growth were investigated. Neither compounds showed significant bioactivities. Copyright © 2012 by Thieme Medical Publishers, Inc.

Park S.J.,RWTH Aachen | Buschmann H.,Sperberweg 15 | Bolm C.,RWTH Aachen
Bioorganic and Medicinal Chemistry Letters | Year: 2011

The syntheses and biological profiles of sulfoximine-based Vioxx® analogs 2 are described. Interesting data have been obtained for 2a, which shows a selective COX-2 inhibition (albeit not as strong as Vioxx® itself) exhibiting reduced hERG activity compare to the parent sulfone Vioxx® (1). © 2011 Elsevier Ltd. All rights reserved.

Park S.J.,RWTH Aachen | Baars H.,RWTH Aachen | Mersmann S.,RWTH Aachen | Buschmann H.,Sperberweg 15 | And 7 more authors.
ChemMedChem | Year: 2013

From insects to cancer: N-Cyano sulfoximines were evaluated for COX inhibition and antiproliferative activity against a panel of cancer cell lines. The most active compound exhibited potent COX-2 inhibition, some selectivity for COX-2 over COX-1, only slight cytotoxicity towards healthy cells (HaCaT skin cells), and no mutagenic potential (as determined by an Ames assay). © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Chen X.Y.,RWTH Aachen | Park S.J.,RWTH Aachen | Buschmann H.,Sperberweg 15 | De Rosa M.,RWTH Aachen | And 2 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

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). © 2012 Elsevier Ltd. All rights reserved.

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