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

被引：5

作者：

Corvino, Angela ^{[1
]}

Rosa, Roberta ^{[2
]}

Incisivo, Giuseppina Maria ^{[1
]}

Fiorino, Ferdinando ^{[1
]}

Frecentese, Francesco ^{[1
]}

Magli, Elisa ^{[1
]}

Perissutti, Elisa ^{[1
]}

Saccone, Irene ^{[1
]}

Santagada, Vincenzo ^{[1
]}

Cirino, Giuseppe ^{[1
]}

Riemma, Maria Antonietta ^{[1
]}

Temussi, Piero A. ^{[3
]}

Ciciola, Paola ^{[2
]}

Bianco, Roberto ^{[2
]}

Caliendo, Giuseppe ^{[1
]}

Roviezzo, Fiorentina ^{[1
]}

Severino, Beatrice ^{[1
]}

机构：

[1] Univ Naples Federico II, Sch Med, Dept Pharm, I-80131 Naples, Italy

[2] Univ Naples Federico II, Div Oncol, Dept Clin Med & Surg, I-80131 Naples, Italy

[3] Kings Coll London, Wohl Inst, 5 Cutcombe Rd, London SE5 9RT, England

来源：

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | 2017年 / 18卷 / 11期

关键词：

Sphingosine Kinase 1; Sphingosine Kinase 2; inhibitors; synthesis; antiproliferative activity; CANCER; DESIGN; SPHK;

D O I：

10.3390/ijms18112332

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

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页数：18

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