New dual inhibitors of EGFR and HER2 protein tyrosine kinases

被引：46

作者：

Fink, BE

Vite, GD

Mastalerz, H

Kadow, JF

Kim, SH

Leavitt, KJ

Du, K

Crews, D

Wong, TW

Hunt, JT

Vyas, DM

Tokarski, JS

机构：

[1] Bristol Myers Squibb Pharmaceut Res Inst, Dept Oncol Chem, Princeton, NJ 08543 USA

[2] Bristol Myers Squibb Pharmaceut Res Inst, Dept Discovery Biol, Princeton, NJ 08543 USA

[3] Bristol Myers Squibb Pharmaceut Res Inst, Dept Comp Aided Design, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 21期

关键词：

panHER; EGFR; kinase inhibitor;

D O I：

10.1016/j.bmcl.2005.07.027

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of dual EGFR and HER2 inhibitors based on the pyrrolo[2,1-f][1,2,4]triazine nucleus is described. A general route toward their synthesis, which enables functionalization at multiple sites, has been developed. Biological evaluation in enzymatic and cell-based assays has identified a series of C-6 carbamates with potent biochemical and cellular activities.

引用

页码：4774 / 4779

页数：6

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