Synthesis of selective inhibitors of sphingosine kinase 1

被引：49

作者：

Baek, Dong Jae ^{[1
]}

MacRitchie, Neil ^{[2
]}

Pyne, Nigel J. ^{[2
]}

Pyne, Susan ^{[2
]}

Bittman, Robert ^{[1
]}

机构：

[1] CUNY Queens Coll, Dept Chem & Biochem, Flushing, NY 11367 USA

[2] Univ Strathclyde, Cell Biol Grp, Strathclyde Inst Pharm & Biomed Sci, Glasgow G4 0RE, Lanark, Scotland

来源：

CHEMICAL COMMUNICATIONS | 2013年 / 49卷 / 21期

关键词：

SMOOTH-MUSCLE; PROTEASOMAL-DEGRADATION; BREAST-CANCER; EXPRESSION; SPHINGOSINE-1-PHOSPHATE; SURVIVAL; FTY720; CELLS;

D O I：

10.1039/c3cc00181d

中图分类号：

O6 [化学];

学科分类号：

070301 [无机化学];

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.

引用

页码：2136 / 2138

页数：3

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