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Bioorg Med Chem Lett. 2012 Oct 15;22(20):6368-72. doi: 10.1016/j.bmcl.2012.08.075. Epub 2012 Aug 27.

Multisubstituted quinoxalines and pyrido[2,3-d]pyrimidines: synthesis and SAR study as tyrosine kinase c-Met inhibitors.

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1
Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.

Abstract

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 IC(50) value of 6.5 nM. Further structural modifications based on this compound were undergoing.

PMID:
22985853
DOI:
10.1016/j.bmcl.2012.08.075
[Indexed for MEDLINE]
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