New pyrazolo[3,4-d]pyrimidines endowed with A431 antiproliferative activity and inhibitory properties of Src phosphorylation

New pyrazolo[3,4-d]pyrimidines endowed with A431 antiproliferative activity and inhibitory properties of Src phosphorylation
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DOI:
10.1016/j.bmcl.2004.03.013
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发表时间:
2004-05-17
影响因子:
2.7
通讯作者:
Botta, M
Botta, M
中科院分区:
医学4区
文献类型:
--
作者:
Schenone, S;Bruno, O;Botta, M

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合成了在I位和6位带有不同取代基的4-氨基吡唑并[3,4-d]嘧啶类化合物。新化合物显示出对A431细胞的抗增殖活性,被发现是Src磷酸化的抑制剂,并诱导凋亡性细胞死亡。特别地,2 h是比参考化合物PP 2更好的Src磷酸化抑制剂。(C)2004爱思唯尔有限公司保留所有权利。
New 4-aminopyrazolo[3,4-d]pyrimidines bearing various substituents at the position I and 6, were synthesized. The new compounds showed antiproliferative activity toward A431 cells, were found to be inhibitors of Src phosphorylation, and induced apoptotic cell death. In particular, 2h was a better inhibitor of Src phosphorylation than the reference compound PP2. (C) 2004 Elsevier Ltd. All rights reserved.