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Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity.

Abstract：

:Receptor tyrosine kinase c-Met acts as an alternative angiogenic pathway in the process and contents of cancers. A series of imidazopyridine derivatives were designed and synthesized according to the established docking studies as possible c-Met inhibitors. Most of these imidazopyridine derivatives displayed nanomolar potency against c-Met in both biochemical enzymatic screens and cellular pharmacology studies. Especially, compound 7g exhibited the most inhibitory activity against c-Met with IC50 of 53.4nM and 253nM in enzymatic and cellular level, respectively. Following that, the compound 7g was docked into the protein of c-Met and the structure-activity relationship was analyzed in detail. These findings indicated that the novel imidazopyridine derivative compound 7g was a potential c-Met inhibitor deserving further investigation for cancer treatment.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Yang Y,Zhang Y,Yang L,Zhao L,Si L,Zhang H,Liu Q,Zhou J

doi

10.1016/j.bioorg.2016.12.002

subject

Has Abstract

pub_date

2017-02-01 00:00:00

pages

126-132

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(16)30289-9

journal_volume

70

pub_type

杂志文章

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