Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 4, Issue 8, Pages 806-810Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml400203d
Keywords
Hepatocyte growth factor receptor (HGFR or c-Met); anaplastic lymphoma kinase (ALK); inhibitor; cancer; aminopyridine; aminopyrazine; spiro[indoline-3,4 '-piperidine]-2-one; small molecule
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Funding
- International Science and Technology Cooperation Base of Guangdong Provincial Department of Science and Technology [2009B050900006]
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A series of novel aminopyridyl/pyrazinyl-substituted spiro[indoline-3,4'-piperidine]-2-ones were designed, synthesized, and tested in various in vitro/in vivo pharmacological and antitumor assays. 6-[6-Amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-3-pyridyl]-1'-methylspiro[indoline-3,4'-piperidine]-2-one (compound 5b or SMU-B) was identified as a potent, highly selective, well-tolerated, and orally efficacious c-Met/ALK dual inhibitor, which showed pharmacodynamics effect by inhibiting c-Met phosphorylation in vivo and significant tumor growth inhibitions (>50%) in GTL-16 human gastric carcinoma xenograft models.
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