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Development of 1,2,3-Triazole-Based Sphingosine Kinase Inhibitors and Their Evaluation as Antiproliferative Agents.


ABSTRACT: Two series of N-(aryl)-1-(hydroxyalkyl)pyrrolidine-2-carboxamides (2a-2g and 3a-3g) and 1,4-disubstituted 1,2,3-triazoles (5a-5h and 8a-8h) were synthesized. All the compounds, containing a lipophilic tail and a polar headgroup, were evaluated as sphingosine kinase (SphK) inhibitors by assessing their ability to interfere with the acetylcholine (Ach) induced relaxation of aortic rings pre-contracted with phenylephrine. Moreover, their antiproliferative activity was tested on several cell lines expressing both SphK1 and SphK2. Compounds 5h and 8f, identified as the most efficient antiproliferative agents, showed a different selectivity profile, with 8f being selective for SphK1.

SUBMITTER: Corvino A 

PROVIDER: S-EPMC5713301 | biostudies-literature | 2017 Nov

REPOSITORIES: biostudies-literature

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Two series of <i>N</i>-(aryl)-1-(hydroxyalkyl)pyrrolidine-2-carboxamides (<b>2a</b>-<b>2g</b> and <b>3a</b>-<b>3g</b>) and 1,4-disubstituted 1,2,3-triazoles (<b>5a</b>-<b>5h</b> and <b>8a</b>-<b>8h</b>) were synthesized. All the compounds, containing a lipophilic tail and a polar headgroup, were evaluated as sphingosine kinase (SphK) inhibitors by assessing their ability to interfere with the acetylcholine (Ach) induced relaxation of aortic rings pre-contracted with phenylephrine. Moreover, thei  ...[more]

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