Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors
Weike Liao
1
,
Gang Hu
1
,
Zhuang Guo
1
,
Deyu Sun
2
,
Lixia Zhang
1
,
Yanxin Bu
1
,
Yingxiu Li
1
,
Yajing Liu
1
,
Ping Gong
1
2
Liaoning Cancer Hospital & Institute, 44 Xiaoheyan Road, Dadong District, PR China.
|
Publication type: Journal Article
Publication date: 2015-08-01
scimago Q2
wos Q1
SJR: 0.608
CiteScore: 6.7
Impact factor: 3.0
ISSN: 09680896, 14643391
PubMed ID:
26169763
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
A series of 4-(2-fluorophenoxy)quinoline derivatives containing an imidazolone moiety were designed, synthesized and evaluated for their in vitro biological activities against c-Met kinase and four cancer cell lines (A549, H460, HT-29 and MKN-45). Most compounds showed moderate to excellent activities in enzyme and cellular assays. The most promising analog, 58 (c-Met IC50=1.42 nM), displayed 2.1-, 8.6-fold increase against H460, and MKN-45 cell lines, respectively, compared with foretinib. An analysis of structure-activity relationships revealed that an ortho substituted phenyl ring as well as an N-unsubstituted imidazolone linker is favorable for antitumor activity.
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Citations from 2025:
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GOST
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Liao W. et al. Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors // Bioorganic and Medicinal Chemistry. 2015. Vol. 23. No. 15. pp. 4410-4422.
GOST all authors (up to 50)
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Liao W., Hu G., Guo Z., Sun D., Zhang L., Bu Y., Li Y., Liu Y., Gong P. Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors // Bioorganic and Medicinal Chemistry. 2015. Vol. 23. No. 15. pp. 4410-4422.
Cite this
RIS
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TY - JOUR
DO - 10.1016/j.bmc.2015.06.026
UR - https://doi.org/10.1016/j.bmc.2015.06.026
TI - Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors
T2 - Bioorganic and Medicinal Chemistry
AU - Liao, Weike
AU - Hu, Gang
AU - Guo, Zhuang
AU - Sun, Deyu
AU - Zhang, Lixia
AU - Bu, Yanxin
AU - Li, Yingxiu
AU - Liu, Yajing
AU - Gong, Ping
PY - 2015
DA - 2015/08/01
PB - Elsevier
SP - 4410-4422
IS - 15
VL - 23
PMID - 26169763
SN - 0968-0896
SN - 1464-3391
ER -
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BibTex (up to 50 authors)
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@article{2015_Liao,
author = {Weike Liao and Gang Hu and Zhuang Guo and Deyu Sun and Lixia Zhang and Yanxin Bu and Yingxiu Li and Yajing Liu and Ping Gong},
title = {Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors},
journal = {Bioorganic and Medicinal Chemistry},
year = {2015},
volume = {23},
publisher = {Elsevier},
month = {aug},
url = {https://doi.org/10.1016/j.bmc.2015.06.026},
number = {15},
pages = {4410--4422},
doi = {10.1016/j.bmc.2015.06.026}
}
Cite this
MLA
Copy
Liao, Weike, et al. “Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors.” Bioorganic and Medicinal Chemistry, vol. 23, no. 15, Aug. 2015, pp. 4410-4422. https://doi.org/10.1016/j.bmc.2015.06.026.