Potent, low-calcemic, selective inhibitors of CYP24 hydroxylase: 24-sulfone analogs of the hormone 1alpha,25-dihydroxyvitamin D3.
The new 24-phenylsulfone 4a, a low-calcemic analog of the natural hormone 1alpha,25-dihydroxyvitamin D(3), is a potent (IC(50) = 28nM) and highly selective inhibitor of the human 24-hydroxylase enzyme CYP24.
Posner
Gary H
GH
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 N. Charles Street, Baltimore, MD 21218-2685, USA. ghp@jhu.edu
Crawford
Kenneth R
KR
Yang
Hong Woon
HW
Kahraman
Mehmet
M
Jeon
Heung Bae
HB
Li
Hongbin
H
Lee
Jae Kyoo
JK
Suh
Byung Chul
BC
Hatcher
Mark A
MA
Labonte
Tanzina
T
Usera
Aimee
A
Dolan
Patrick M
PM
Kensler
Thomas W
TW
Peleg
Sara
S
Jones
Glenville
G
Zhang
Anqi
A
Korczak
Bozena
B
Saha
Uttam
U
Chuang
Samuel S
SS
D000818:Animals; D002117:Calcitriol / Q000031:analogs & derivatives / Q000494:pharmacology*; D002460:Cell Line; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D013057:Spectrum Analysis; D013250:Steroid Hydroxylases / Q000037:antagonists & inhibitors*; D013450:Sulfones / Q000737:chemistry*; D014158:Transcription, Genetic / Q000187:drug effects; D065668:Vitamin D3 24-Hydroxylase
D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors; D013450:Sulfones; D013250:Steroid Hydroxylases; D065668:Vitamin D3 24-Hydroxylase; D002117:Calcitriol