- Removal of the 26-Methyl Group from 19-nor-1 alpha,25-Dihydroxyvitamin D-3 Markedly Reduces in Vivo Calcemic Activity without Altering in Vitro VDR Binding, HL-60 Cell Differentiation, and Transcription
[作者:GRZYWACZ PAWEL; CHIELLINI GRAZIA; PLUM LORI A; CLAGETTDAME MARGARET; DELUCA HECTOR F,期刊:Journal of Medicinal Chemistry, 页码:8642-8649 , 文章类型: Article,,卷期:2010年53-24]
- Twelve new analogues of 19-nor-1 alpha,25-dihydroxyvitamin D-3 (5-16) were prepared by convergent syntheses, employing the Wittig-Horner reaction. The necessary Grundmann type ketones (45-48), possessing fixed configurat...
- Inhibition of Sphingosine 1-Phosphate Lyase for the Treatment of Rheumatoid Arthritis: Discovery of (E)-1-(4((1R,2S,3R)-1,2,3,4-Tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone Oxime (LX2931) and (1R,2S,3R)-1-(2-(Isoxazol-3-yl)-1H-imidazol-4-yl)butane-1,2,3,4-tetraol (LX2932)
[作者:BAGDANOFF JEFFREY T; DONOVIEL MICHAEL S; NOURALDEEN AMR; CARLSEN MARIANNE; JESSOP THEODORE C; TARVER JAMES; ALEEM SAADAT; DONG LI; ZHANG HAIMING; BOTEJU LAKMAL; HAZELWOOD JILL; YAN JACK; BEDNARZ MARK; LAYEK SUMAN; OWUSU IRIS B; GOPINATHAN SUMA; MORAN LIAM; LAI ZHONG; KRAMER JEFF; KIMBALL S DAVID; YALAMANCHILI PADMAJA; HEYDORN WILLIAM E; FRAZIER KENNY S; BROOKS BARBARA; BROWN PHILIP; WILSON ALAN; SONNENBURG WILLIAM K; MAIN ALAN; CARSON KENNETH G; ORAVECZ TAMAS; AUGERI DAVID J,期刊:Journal of Medicinal Chemistry, 页码:8650-8662 , 文章类型: Article,,卷期:2010年53-24]
- Sphingosine 1-phosphate lyase (S1PL) has been characterized as a novel target for the treatment of autoimmune disorders using genetic and pharmacological methods. Medicinal chemistry efforts targeting S1PL by direct in v...
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