Potent and Selective Inhibitors of the AbL-Kinase: Phenylaminopyrimidine (PAP) Derivatives.
Potent and Selective Inhibitors of the AbL-Kinase: Phenylaminopyrimidine (PAP) Derivatives.
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AbL 激酶的强效选择性抑制剂：苯氨基嘧啶 (PAP) 衍生物。
DOI：
10.1002/chin.199720134
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发表时间：
1997
期刊：
影响因子：
--
通讯作者：
N. Lydon
中科院分区：
文献类型：
--
作者：
J. Zimmermann;E. Buchdunger;H. Mett;T. Meyer;N. Lydon
由于其相对明确的病因，慢性髓性白血病（CML）是使用Bcr-Abl酪氨酸蛋白激酶选择性抑制剂治疗的理想疾病靶点。苯胺嘧啶类的广泛优化产生了高效和选择性的Bcr-Abl激酶抑制剂。化合物1在体外水平上对Abl酪氨酸蛋白激酶具有较高的效价（IC50= 38 nM）和选择性。
Due to its relatively clear etiology, Chronic myelogenous leukemia (CML) represents an ideal disease target for a therapy using a selective inhibitor of the Bcr-Abl tyrosine protein kinase. Extensive optimization of the class of phenylamino-pyrimidines yielded highly potent and selective Bcr-Abl kinase inhibitors. Compound 1 shows high potency (IC50= 38 nM) and selectivity for the Abl tyrosine protein kinase at the in vitro level.