Synthesis of (S)-FTY720 vinylphosphonate analogues and evaluation of their potential as sphingosine kinase 1 inhibitors and activators

…, N MacRitchie, S Pyne, NJ Pyne, R Bittman

文献索引：Liu, Zheng; Macritchie, Neil; Pyne, Susan; Pyne, Nigel J.; Bittman, Robert Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 9 p. 2503 - 2510

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被引用次数: 19

摘要

Sphingosine kinase 1 (SK1) is over-expressed in many cancers where it provides a selective growth and survival advantage to these cells. SK1 is thus a target for anti-cancer agents that can promote apoptosis of cancer cells. In previous work, we synthesized a novel allosteric SK1 inhibitor,(S)-FTY720 vinylphosphonate. We now report a more expeditious route to this inhibitor which features B-alkyl Suzuki coupling as a key step and show that ...