Abstract:
:Five novel 1H-pyrrolo[2,3-b]pyridine or 1H-pyrazolo[3,4-b]pyridine derivatives, with a methylene, sulfur, sulfoxide or cyclopropyl group as a linker, were designed, synthesized and biologically evaluated against c-Met and ALK. The development of these methods of compound synthesis may provide an important reference for the construction of novel 7-azaindole and 7-azaindazole derivatives with a single atom linker. The enzyme assay and cell assay in vitro showed that compound 9 displayed strong c-Met kinase inhibition with IC50 of 22.8nM, moderate ALK kinase inhibition, and strong cell inhibition with MKN-45 IC50 of 329nM and EBC-1 IC50 of 479nM. In order to find the better candidate compounds, compounds 8, 9 and 10 have been selected as tool compounds for further optimization.
journal_name
Bioorg Chemjournal_title
Bioorganic chemistryauthors
Liu N,Wang Y,Huang G,Ji C,Fan W,Li H,Cheng Y,Tian Hdoi
10.1016/j.bioorg.2016.02.009subject
Has Abstractpub_date
2016-04-01 00:00:00pages
146-58eissn
0045-2068issn
1090-2120pii
S0045-2068(16)30018-9journal_volume
65pub_type
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