期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 11, 页码 5520-5526出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.08.067
关键词
Pyrazolo[3,4-g]quinoxaline; Kinase inhibition; In vitro antiproliferative activities
资金
- French Ministere de l'Enseignement Superieur et de la Recherche
- ANR [ANR-08-JCJC-0131-CSD 3]
- Region Auvergne Synbio Project
- Agence Nationale de la Recherche (ANR) [ANR-08-JCJC-0131] Funding Source: Agence Nationale de la Recherche (ANR)
The synthesis of new pyrazolo[3,4-g]quinoxaline derivatives, as well as their Pim kinases (Pim-1, Pim-2, Pim-3) inhibitory potencies and in vitro antiproliferative activities toward a human fibroblast primary culture and three human solid cancer cell lines (PA1, PC3 and DU145) are described. The results obtained in this preliminary structure activity relationship study have pointed out that most of the compounds in this series exhibited interesting in vitro Pim-3 kinase inhibitory potencies. Moreover, some of the tested compounds have demonstrated favorable antiproliferative potencies. (C) 2010 Elsevier Masson SAS. All rights reserved.
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