Synthesis and biological evaluation of 3,6-diamino-1H-pyrazolo[3,4-b]pyridine derivatives as protein kinase inhibitors
Synthesis and biological evaluation of 3,6-diamino-1H-pyrazolo[3,4-b]pyridine derivatives as protein kinase inhibitors
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DOI：
10.1016/j.bmcl.2009.06.099
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发表时间：
2009-08-15
影响因子：
2.7
通讯作者：
Marco-Contelles, Jose
中科院分区：
文献类型：
--
作者：
Chioua, Mourad;Samadi, Abdelouahid;Marco-Contelles, Jose
报道了一系列不同取代的3，6-二氨基-1H-吡唑并[3，4-B]吡啶衍生物的合成和生物活性评价。从对选择的疾病相关蛋白激酶的抑制结果[IC 50（μ M）DYRK 1A = 11; CDK 5 = 0.41; GSK-3 = 1.5]中，我们观察到3，6-二氨基-4-苯基-1H-吡唑并[3，4-B]吡啶-5-腈（4）在寻找治疗阿尔茨海默病的药物中构成潜在的新的和简单的先导化合物。(C)2009爱思唯尔有限公司保留所有权利。
The synthesis and biological evaluation of a number of differently substituted 3,6-diamino-1H-pyrazolo[3,4-b] pyridine derivatives are reported. From the inhibition results on a selection of disease-relevant protein kinases [IC50 (mu M) DYRK1A = 11; CDK5 = 0.41; GSK-3 = 1.5] we have observed that 3,6-diamino-4-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (4) constitutes a potential new and simple lead compound in the search of drugs for the treatment of Alzheimer's disease. (C) 2009 Elsevier Ltd. All rights reserved.