Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives

…, I Fellows, ND D'Angelo, C Dominguez…

文献索引：Norman, Mark H.; Liu, Longbin; Lee, Matthew; Xi, Ning; Fellows, Ingrid; D'Angelo, Noel D.; Dominguez, Celia; Rex, Karen; Bellon, Steven F.; Kim, Tae-Seong; Dussault, Isabelle Journal of Medicinal Chemistry, 2012 , vol. 55, # 5 p. 1858 - 1867

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被引用次数: 40

摘要

Deregulation of c-Met receptor tyrosine kinase activity leads to tumorigenesis and metastasis in animal models. More importantly, the identification of activating mutations in c- Met, as well as MET gene amplification in human cancers, points to c-Met as an important target for cancer therapy. We have previously described two classes of c-Met kinase inhibitors (class I and class II) that differ in their binding modes and selectivity profiles. The ...