Potent, Selective and Low-Calcemic Inhibitors of CYP24 Hydroxylase: 24-Sulfoximine Analogues of the Hormone 1α,25-Dihydroxyvitamin D3
Journal of Medicinal Chemistry2004Vol. 47(27), pp. 6854–6863
Citations Over TimeTop 10% of 2004 papers
Mehmet Kahraman, Sandra Sinishtaj, Patrick M. Dolan, Thomas W. Kensler, Sara Peleg, Uttam Kumar Saha, Samuel S. Chuang, Galina Bernstein, Bożena Korczak, Gary H. Posner
Abstract
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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