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pubmed-article:15615534pubmed:abstractTextA dozen 24-sulfoximine analogues of the hormone 1alpha,25-dihydroxyvitamin D(3) were prepared, differing not only at the stereogenic sulfoximine stereocenter but also at the A-ring. Although these sulfoximines were not active transcriptionally and were only very weakly antiproliferative, some of them are powerful hydroxylase enzyme inhibitors. Specifically, 24-(S)-NH phenyl sulfoximine 3a is an extremely potent CYP24 inhibitor (IC(50) = 7.4 nM) having low calcemic activity. In addition, this compound shows high selectivity toward the CYP24 enzyme in comparison to CYP27A1 (IC(50) > 1000 nM) and CYP27B (IC(50) = 554 nM).lld:pubmed
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pubmed-article:15615534pubmed:articleTitlePotent, selective and low-calcemic inhibitors of CYP24 hydroxylase: 24-sulfoximine analogues of the hormone 1alpha,25-dihydroxyvitamin D(3).lld:pubmed
pubmed-article:15615534pubmed:affiliationDepartment of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, MD 21218, USA.lld:pubmed
pubmed-article:15615534pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:15615534pubmed:publicationTypeResearch Support, U.S. Gov't, P.H.S.lld:pubmed
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