Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors
Journal Article
·
· Bioorg. Med. Chem. Lett.
- BMS
Biarylamine-based inhibitors of Met kinase have been identified. Lead compounds demonstrate nanomolar potency in Met kinase biochemical assays and significant activity in the Met-driven GTL-16 human gastric carcinoma cell line. X-ray crystallography revealed that these compounds adopt a bioactive conformation, in the kinase domain, consistent with that previously seen with 2-pyridone-based Met kinase inhibitors. Compound 9b demonstrated potent in vivo antitumor activity in the GTL-16 human tumor xenograft model.
- Research Organization:
- Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
- Sponsoring Organization:
- USDOE
- OSTI ID:
- 1002642
- Journal Information:
- Bioorg. Med. Chem. Lett., Vol. 20, Issue (9) ; 05, 2010; ISSN 0960-894X
- Country of Publication:
- United States
- Language:
- ENGLISH
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