期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 24, 期 18, 页码 4281-4290出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2016.07.019
关键词
c-Met inhibitors; Imidazo[4,5-b]pyrazines; Docking study; Structure-activity relationship
Aberrant c-Met activation has been implicated in multiple tumor oncogenic processes and drug resistance. In this study, a series of imidazo[4,5-b]pyrazine derivatives was designed and synthesized, and their inhibitory activities were evaluated in vitro. Structure-activity relationship (SAR) was investigated systematically and docking analysis was performed to elucidate the binding mode, leading to the identification of the most promising compound 1D-2 which exhibited significant inhibitory effect on both enzymatic (IC50 = 1.45 nM) and cellular (IC50 = 24.7 nM in H1993 cell line) assays, as well as exquisite selectivity and satisfactory metabolic stability in human and rat liver microsomes. (C) 2016 Elsevier Ltd. All rights reserved.
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