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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
27
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pubmed:dateCreated |
2004-12-23
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pubmed:abstractText |
A 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).
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
30
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pubmed:volume |
47
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6854-63
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pubmed:dateRevised |
2008-8-16
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pubmed:meshHeading |
pubmed-meshheading:15615534-Animals,
pubmed-meshheading:15615534-Calcitriol,
pubmed-meshheading:15615534-Calcium,
pubmed-meshheading:15615534-Cytochrome P-450 Enzyme System,
pubmed-meshheading:15615534-Male,
pubmed-meshheading:15615534-Rats,
pubmed-meshheading:15615534-Rats, Inbred F344,
pubmed-meshheading:15615534-Steroid Hydroxylases,
pubmed-meshheading:15615534-Structure-Activity Relationship,
pubmed-meshheading:15615534-Sulfones
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pubmed:year |
2004
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pubmed:articleTitle |
Potent, selective and low-calcemic inhibitors of CYP24 hydroxylase: 24-sulfoximine analogues of the hormone 1alpha,25-dihydroxyvitamin D(3).
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pubmed:affiliation |
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, MD 21218, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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