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Article

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

1
Department of Pharmacy, School of Medicine, University of Naples Federico II, 80131 Naples, Italy
2
Department of Clinical Medicine and Surgery, Oncology Division, University of Naples Federico II, 80131 Naples, Italy
3
The Wohl Institute, King’s College London, 5 Cutcombe Rd, London SE5 9RT, UK
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2017, 18(11), 2332; https://doi.org/10.3390/ijms18112332
Received: 19 October 2017 / Revised: 31 October 2017 / Accepted: 1 November 2017 / Published: 5 November 2017
(This article belongs to the Special Issue Sphingolipids: Signals and Disease)
Two series of N-(aryl)-1-(hydroxyalkyl)pyrrolidine-2-carboxamides (2a2g and 3a3g) and 1,4-disubstituted 1,2,3-triazoles (5a5h and 8a8h) 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. View Full-Text
Keywords: Sphingosine Kinase 1; Sphingosine Kinase 2; inhibitors; synthesis; antiproliferative activity Sphingosine Kinase 1; Sphingosine Kinase 2; inhibitors; synthesis; antiproliferative activity
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MDPI and ACS Style

Corvino, A.; Rosa, R.; Incisivo, G.M.; Fiorino, F.; Frecentese, F.; Magli, E.; Perissutti, E.; Saccone, I.; Santagada, V.; Cirino, G.; Riemma, M.A.; Temussi, P.A.; Ciciola, P.; Bianco, R.; Caliendo, G.; Roviezzo, F.; Severino, B. Development of 1,2,3-Triazole-Based Sphingosine Kinase Inhibitors and Their Evaluation as Antiproliferative Agents. Int. J. Mol. Sci. 2017, 18, 2332. https://doi.org/10.3390/ijms18112332

AMA Style

Corvino A, Rosa R, Incisivo GM, Fiorino F, Frecentese F, Magli E, Perissutti E, Saccone I, Santagada V, Cirino G, Riemma MA, Temussi PA, Ciciola P, Bianco R, Caliendo G, Roviezzo F, Severino B. Development of 1,2,3-Triazole-Based Sphingosine Kinase Inhibitors and Their Evaluation as Antiproliferative Agents. International Journal of Molecular Sciences. 2017; 18(11):2332. https://doi.org/10.3390/ijms18112332

Chicago/Turabian Style

Corvino, Angela, Roberta Rosa, Giuseppina M. Incisivo, Ferdinando Fiorino, Francesco Frecentese, Elisa Magli, Elisa Perissutti, Irene Saccone, Vincenzo Santagada, Giuseppe Cirino, Maria A. Riemma, Piero A. Temussi, Paola Ciciola, Roberto Bianco, Giuseppe Caliendo, Fiorentina Roviezzo, and Beatrice Severino. 2017. "Development of 1,2,3-Triazole-Based Sphingosine Kinase Inhibitors and Their Evaluation as Antiproliferative Agents" International Journal of Molecular Sciences 18, no. 11: 2332. https://doi.org/10.3390/ijms18112332

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