Journal
HELVETICA CHIMICA ACTA
Volume 95, Issue 2, Pages 320-326Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/hlca.201100226
Keywords
c-Met Inhibitor; 1H-Pyrido[4; 3-b]indoles; 2; 3; 4; 5-tetrahydro-; Suzuki coupling reaction; Inhibitors; Tyrosine-kinase receptor
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Funding
- Guangdong Provincial Department of Science and Technology [2009B050900006]
- Science and Technology Bureau of Guangzhou [2009A1-E011-8, 2010 V1-E00531-3]
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Since deregulation of the tyrosine-kinase receptor c-Met is implicated in several human cancers and is an attractive target for small-molecule-drug discovery, we report herein the synthesis of 2,3,4,5-tetrahydro-8-[1-(quinolin-6-ylmethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrido[4,3-b]indoles 4a4c and 2,3,4,5-tetrahydro-8-[3-(quinolin-6-ylmethyl)-1,2,4-triazolo[4,3-b]pyridazin-6-yl]-1H-pyrido[4,3-b]indoles 5a5c. These indole derivatives demonstrated inhibition of c-Met kinase activity. Concurrently, five key intermediates were synthesized. These compounds could be prepared in good yields.
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