Title of article
Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors
Author/Authors
Zhen-wei Cai، نويسنده , , Donna Wei، نويسنده , , Gretchen M. Schroeder، نويسنده , , Lyndon A.M. Cornelius، نويسنده , , Kyoung Kim، نويسنده , , Xiao-Tao Chen، نويسنده , , Robert J. Schmidt، نويسنده , , David K. Williams، نويسنده , , John S. Tokarski، نويسنده , , Yongmi An، نويسنده , , John S. Sack، نويسنده , , Veeraswamy Manne، نويسنده , , Amrita Kamath، نويسنده , , Yueping Zhang، نويسنده , , Punit Marathe، نويسنده , , John T. Hunt، نويسنده , , Louis J. Lombardo، نويسنده , , Joseph Fargnoli، نويسنده , , Robert M. Borzilleri، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
6
From page
3224
To page
3229
Abstract
A series of acylurea analogs derived from pyrrolopyridine and aminopyridine scaffolds were identified as potent inhibitors of Met kinase activity. The SAR at various positions of the two kinase scaffolds was investigated. These studies led to the discovery of compounds 3b and 20b, which demonstrated favorable pharmacokinetic properties in mice and significant antitumor activity in a human gastric carcinoma xenograft model.
Keywords
Receptor tyrosine kinase , Protein kinase inhibitors , Met
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799535
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