Synthesis of selective inhibitors of sphingosine kinase 1.

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 (IC(50) = 3.6 μM), which also induced proteasomal degradation of SK1 in human pulmonary arterial smooth muscle cells.

SUBMITTER: Baek DJ 

PROVIDER: S-EPMC3608193 | biostudies-literature | 2013 Mar

REPOSITORIES: biostudies-literature