Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 47, Issue 27, Pages 6854-6863Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm040129+
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Funding
- NCI NIH HHS [CA 93547, CA 52857] Funding Source: Medline
- NIDDK NIH HHS [DK 50583] Funding Source: Medline
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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 (IC50 = 7.4 nM) having low calcemic activity. In addition, this compound shows high selectivity toward the CYP24 enzyme in comparison to CYP27A1 (IC50 > 1000 nM) and CYP27B (IC50 = 554 nM).
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