| Aroyl hydrazones of 2-phenylindole-3-carbaldehydes as novel antimitotic agents. | |
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MedLine Citation:
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PMID: 18513974 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Cell cycle arrest of malignant cells is an important option for cancer treatment. In this study, we modified the structure of antimitotic 2-phenylindole-3-carbaldehydes by condensation with hydrazides of various benzoic and pyridine carboxylic acids. The resulting hydrazones inhibited the growth of MDA-MB 231 and MCF-7 breast cancer cells with IC(50) values of 20-30 nM for the most potent derivatives. These 2-phenylindole derivatives also exerted an inhibitory effect on the growth of both proliferating and resting U-373 MG glioblastoma cells. Though the hydrazones exhibited similar structure-activity relationships as the aldehydes, they did not inhibit tubulin polymerization as the aldehydes but were capable of blocking the cell cycle in G(2)/M phase. The cell cycle arrest was accompanied by apoptosis as demonstrated by the activation of caspase-3. Since these 2-phenylindole-based hydrazones display no structural similarity with other antitumor drugs they are interesting candidates for further development. |
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Authors:
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Susanne Vogel; Doris Kaufmann; Michaela Pojarová; Christine Müller; Tobias Pfaller; Sybille Kühne; Patrick J Bednarski; Erwin von Angerer |
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Publication Detail:
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Type: Journal Article Date: 2008-05-03 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: 16 ISSN: 1464-3391 ISO Abbreviation: Bioorg. Med. Chem. Publication Date: 2008 Jun |
Date Detail:
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Created Date: 2008-06-13 Completed Date: 2008-07-15 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: 6436-47 Citation Subset: IM |
Affiliation:
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Institut für Pharmazie, Universität Regensburg, D-93040 Regensburg, Germany. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Antimitotic Agents
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chemical synthesis,
chemistry*,
pharmacology* Benzoic Acids / chemistry Caspase 3 / metabolism Cell Cycle / drug effects Cell Line, Tumor Cell Proliferation / drug effects* Humans Hydrazones / chemical synthesis, chemistry*, pharmacology* Indoles / chemistry* Pyridines / chemistry |
| Chemical | |
Reg. No./Substance:
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0/Antimitotic Agents; 0/Benzoic Acids; 0/Hydrazones; 0/Indoles; 0/Pyridines; EC 3.4.22.-/Caspase 3 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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