期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 69, 期 -, 页码 77-89出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.08.019
关键词
Synthesis; Quinoline derivatives; c-Met; Antiproliferative activity
资金
- Program for Innovative Research Team of the Ministry of Education of the People's Republic of China
- Program for Liaoning Innovative Research Team in University
Two series of quinoline derivatives bearing the pyridine/pyrimidine scaffold were synthesized, and evaluated for their c-Met kinase inhibitory activity and antiproliferative activity against 5 cancer cell lines (HT-29, H460, MKN-45, A549, and U87MG) were evaluated in vitro. Most compounds showed moderate to excellent potency, and compared to foretinib, the most promising analog 18b (c-Met half-maximal inhibitory concentration [IC50] = 1.39 nM) showed a 7.3-fold increase in activity against HT-29 cell line in vitro. Structure activity relationship studies indicated that regulation of the electron density on the pyridine/pyrimidine ring to a proper degree was a key factor in improving the antitumor activity. (C) 2013 Elsevier Masson SAS. All rights reserved.
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