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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 ?M), 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

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Synthesis of selective inhibitors of sphingosine kinase 1.

Baek Dong Jae DJ MacRitchie Neil N Pyne Nigel J NJ Pyne Susan S Bittman Robert R

Chemical communications (Cambridge, England) 20130207 21

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. ...[more]

PMID: 23388656

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