4.5 Article

Design, synthesis, and biological evaluation of 4-phenoxyquinoline derivatives as potent c-Met kinase inhibitor

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 29, Issue 23, Pages -

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.126666

Keywords

Synthesis; 4-Phenoxyquinoline derivatives; c-Met inhibitors; Antitumor activity

Funding

  1. National Natural Science Foundation of China and LiaoNing Revitalization Talents Program [81573295]
  2. [XLYC1808037]

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A series of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydro-quinoxaline moiety were synthesized and evaluated for their antiproliferative activity against five human cancer cell lines (A549, H460, HT29, MKN-45 and U87MG) in vitro. Most of the tested compounds exhibited more potent inhibitory activities than the positive control foretinib. Compound 1b, 1s and 1t were further examined for their inhibitory activity against c-Met kinase. The most promising compound 1s (with c-Met IC50 value of 1.42 nM) showed remarkable cytotoxicity against A549, H460, HT-29, MKN45 and U87MG cell lines with IC50 values of 0.39 mu M, 0.18 mu M, 0.38 mu M, 0.81 mu M, respectively. Their preliminary structure-activity relationships (SARs) study indicated that the replacement of the aromatic ring with the cyclohexane improved their antiproliferative activity.

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