Abstract:
: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.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
Li J,Wu N,Tian Y,Zhang J,Wu Sdoi
10.1021/ml400203dsubject
Has Abstractpub_date
2013-07-12 00:00:00pages
806-10issue
8issn
1948-5875journal_volume
4pub_type
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