Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 146, Issue -, Pages 368-380Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.01.061
Keywords
1, 3-Thiazolidin-4-one; Urea; Anticancer; Tyrosine kinase; Inhibitors
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Funding
- National Natural Science Foundation of China [21562053]
- Science and Technology Foundation of Guizhou Province [Qian Ke He J Zi [2014]2181]
- Science and Technology Cooperation Plan of Guizhou Province [Qian Ke He LH Zi [2015]7523]
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A total of 29 novel compounds bearing N-1-(2-aryl-1, 3-thiazolidin-4-one)-N-3-aryl ureas were designed, synthesized and evaluated for their biological activities. The structure-activity relationships (SARs) and binding modes of this series of compounds were clarified together. Compound 29b was identified possessing high potency against multi-tyrosine kinases including Ron, c-Met, c-Kit, KDR, Src and IGF-1R, etc. In vitro antiproliferation and cytotoxicity of compound 29b against A549 cancer cell line were confirmed by IncuCyte live-cell imaging. (C) 2018 Elsevier Masson SAS. All rights reserved.
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