Synthesis and biological activities of pyrazolo[3,4-g]quinoxaline derivatives
Synthesis and biological activities of pyrazolo[3,4-g]quinoxaline derivatives
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DOI：
10.1016/j.ejmech.2010.08.067
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发表时间：
2010-11-01
影响因子：
6.7
通讯作者：
Moreau, Pascale
中科院分区：
文献类型：
--
作者：
Gavara, Laurent;Saugues, Emmanuelle;Moreau, Pascale
本发明描述了新的吡唑并[3，4-g]喹喔啉衍生物的合成，以及它们的Pim激酶（Pim-1、Pim-2、Pim-3）抑制效力和对人成纤维细胞原代培养物和三种人实体癌细胞系（PA 1、PC 3和DU 145）的体外抗增殖活性。初步构效关系研究结果表明，该系列化合物中的大部分化合物均具有体外Pim-3激酶抑制活性。此外，一些测试的化合物已经证明了有利的抗增殖效力。(C)2010年Elsevier Masson SAS。All rights reserved.
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.