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Title: Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors

Journal Article · · Bioorg. Med. Chem. Lett.

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.

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
USDOE
OSTI ID:
1006818
Journal Information:
Bioorg. Med. Chem. Lett., Vol. 18, Issue (11) ; 06, 2008; ISSN 0960-894X
Country of Publication:
United States
Language:
ENGLISH