title: Bioactive sulfoximines: syntheses and properties of Vioxx analogs.
abstract: 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).
authors.affiliation: Institute of Organic Chemistry, RWTH Aachen University, Landoltweg 1, D-52056 Aachen, Germany.
authors.forename: Seong Jun
authors.initials: SJ
authors.lastname: Park
authors.forename: Helmut
authors.initials: H
authors.lastname: Buschmann
authors.forename: Carsten
authors.initials: C
authors.lastname: Bolm
mesh_terms: D051546:Cyclooxygenase 2 / Q000378:metabolism*; D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D051638:Ether-A-Go-Go Potassium Channels / Q000037:antagonists & inhibitors*; D057809:HEK293 Cells; D006801:Humans; D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008717:Methionine Sulfoximine / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D052246:Cyclooxygenase 2 Inhibitors; D051638:Ether-A-Go-Go Potassium Channels; D007783:Lactones; D013450:Sulfones; C116926:rofecoxib; D008717:Methionine Sulfoximine; D051546:Cyclooxygenase 2; C496540:PTGS2 protein, human