| Design, synthesis and biological evaluation of thiazolidinone derivatives as potential EGFR and HER-2 kinase inhibitors. | |
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MedLine Citation:
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PMID: 19914835 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Two series of thiazolidinone derivatives designing for potential EGFR and HER-2 kinase inhibitors have been discovered. Some of them exhibited significant EGFR and HER-2 inhibitory activity. Compound 2-(2-(5-bromo-2-hydroxybenzylidene)hydrazinyl)thiazol-4(5H)-one (12) displayed the most potent inhibitory activity (IC(50)=0.09 microM for EGFR and IC(50)=0.42 microM for HER-2), comparable to the positive control erlotinib. Docking simulation was performed to position compound 12 into the EGFR active site to determine the probable binding model. Antiproliferative assay results indicating that some of the thiazolidinone derivatives own high antiproliferative activity against MCF-7. Compound 12 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent. |
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Authors:
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Peng-Cheng Lv; Chang-Fang Zhou; Jin Chen; Peng-Gang Liu; Kai-Rui Wang; Wen-Jun Mao; Huan-Qiu Li; Ying Yang; Jing Xiong; Hai-Liang Zhu |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2009-10-30 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: 18 ISSN: 1464-3391 ISO Abbreviation: Bioorg. Med. Chem. Publication Date: 2010 Jan |
Date Detail:
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Created Date: 2010-02-03 Completed Date: 2010-04-27 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: England |
Other Details:
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Languages: eng Pagination: 314-9 Citation Subset: IM |
Copyright Information:
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Copyright (c) 2009 Elsevier Ltd. All rights reserved. |
Affiliation:
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State Key Laboratory of Pollution Control and Resource Reuse, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Antineoplastic Agents
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chemical synthesis,
chemistry*,
pharmacology* Cell Line, Tumor Cell Proliferation / drug effects Drug Screening Assays, Antitumor Humans Models, Molecular Neoplasms / drug therapy Protein Binding Protein Kinase Inhibitors / chemical synthesis, chemistry, pharmacology Receptor, Epidermal Growth Factor / antagonists & inhibitors*, chemistry, metabolism Receptor, erbB-2 / antagonists & inhibitors*, metabolism Structure-Activity Relationship Thiazolidines / chemical synthesis, chemistry*, pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents; 0/Protein Kinase Inhibitors; 0/Thiazolidines; EC 2.7.10.1/Receptor, Epidermal Growth Factor; EC 2.7.10.1/Receptor, erbB-2 |
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