Potent and selective inhibitors of the Abl-kinase: Phenylamino-pyrimidine (PAP) derivatives

被引：209

作者：

Zimmermann, J

Buchdunger, E

Mett, H

Meyer, T

Lydon, NB

机构：

[1] Ciba Pharmaceutical Division, Oncology Research Department, Ciba-Geigy Limited

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(96)00601-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 1997, Elsevier Science Ltd.

引用

页码：187 / 192

页数：6

共 13 条

[1]

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[2]

Buchdunger E, 1996, CANCER RES, V56, P100

[3] SELECTIVE-INHIBITION OF THE PLATELET-DERIVED GROWTH-FACTOR SIGNAL-TRANSDUCTION PATHWAY BY A PROTEIN-TYROSINE KINASE INHIBITOR OF THE 2-PHENYLAMINOPYRIMIDINE CLASS [J].