Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 20, Pages 6368-6372Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.08.075
Keywords
c-Met kinase; 3,5-Diamino-7-trifluoroquinoline; hERG; Antitumor activity; Structure-activity relationship (SAR)
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Funding
- Chinese National Science Foundation for the Distinguished Young Scholars Program [81125021]
- Chinese National Science Foundation for the Innovation Research Group [810 21062]
- National Science & Technology Major Project on Key New Drug Creation and Manufacturing Program [2012ZX09103-101-035, 2010ZX09401-401, 2012ZX093010 01-007]
- Shanghai Commission of Science and Technology [10JC1417100, 10dz1910104]
- Hundred Talents Project of Chinese Academy of Sciences
- National Natural Science Foundation of China [81102461]
- National Program on Key Basic Research Project of China [2012CB910704]
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Two series of new analogues were designed by replacing the quinoline scaffold of our earlier lead 2 (zgw-atinib) with quinoxaline and pyrido[2,3-d]pyrimidine frameworks. Moderate c-Met inhibitory activity was observed in the quinoxaline series. Among the pyrido[2,3-d]pyrimidine series, compounds 13a-c possessing an O-linkage were inactive, whilst the N-linked analogues 15a-c retained c-Met inhibitory potency. Highest activity was observed in the 3-nitrobenzyl analog 15b that showed an IC50 value of 6.5 nM. Further structural modifications based on this compound were undergoing. (c) 2012 Elsevier Ltd. All rights reserved.
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