| Synthesis, biological evaluation, and molecular docking studies of 2,6-dinitro-4-(trifluoromethyl)phenoxysalicylaldoxime derivatives as novel antitubulin agents. | |
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MedLine Citation:
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PMID: 22512906 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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A series of 2,6-dinitro-4-(trifluoromethyl)phenoxysalicylaldoxime derivatives (1h-20h) have been designed and synthesized, and their biological activities were also evaluated as potential antiproliferation and tubulin polymerization inhibitors. Among all the compounds, 2h showed the most potent activity in vitro, which inhibited the growth of MCF-7, Hep-G2 and A549 cell lines with IC(50) values of 0.70±0.05, 0.68±0.02 and 0.86±0.05μM, respectively. Compound 2h also exhibited significant tubulin polymerization inhibitory activity (IC(50)=3.06±0.05μM). The result of flow cytometry (FCM) demonstrated that compound 2h induced cell apoptosis. Docking simulation was performed to insert compound 2h into the crystal structure of tubulin at colchicine binding site to determine the probable binding model. Based on the preliminary results, compound 2h with potent inhibitory activity in tumor growth may be a potential anticancer agent. |
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Authors:
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Ting-Ting Zhao; Xiang Lu; Xian-Hui Yang; Li-Ming Wang; Xi Li; Zhong-Chang Wang; Hai-Bin Gong; Hai-Liang Zhu |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-4-1 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: - ISSN: 1464-3391 ISO Abbreviation: - Publication Date: 2012 Apr |
Date Detail:
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Created Date: 2012-4-19 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2012. Published by Elsevier Ltd. |
Affiliation:
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State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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