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Synthesis of selective inhibitors of sphingosine kinase 1

  作者 BAEK DONG JAE; MACRITCHIE NEIL; PYNE NIGEL J; PYNE SUSAN; BITTMAN ROBERT  
  选自 期刊  Chemical Communications;  卷期  2013年49-21;  页码  2136-2138  
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[摘要]Sphingosine kinase isoform 1 (SK1) inhibitors may serve as therapeutic agents for proliferative diseases, including hypertension. We synthesized a series of sphingosine-based SK1-selective inhibitors, the most potent of which is RB-005 (IC50 = 3.6 mu M), which also induced proteasomal degradation of SK1 in human pulmonary arterial smooth muscle cells.

 
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