Synthesis of selective inhibitors of sphingosine kinase 1

Baek, Dong Jae and MacRitchie, Neil and Pyne, Nigel and Pyne, Susan and Bittman, Robert (2013) Synthesis of selective inhibitors of sphingosine kinase 1. Chemical Communications (London). ISSN 0009-241X

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Abstract

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 lM), which also induced proteasomal degradation of SK1 in human pulmonary arterial smooth muscle cells.