| Conjugates of the fungal cytotoxin illudin M with improved tumour specificity. | |
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MedLine Citation:
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PMID: 18715789 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A simplified procedure for the isolation of gram quantities of illudin M from culture broths of basidiomycete Omphalotus olearius is described. Esters of illudin M with docosahexaenoic acid, chlorambucil, demethylcantharidinic acid (endothall) and 2,2'-bipyridyl-5,5'-dicarboxylic acid were synthesised and tested for cytotoxicity and induction of apoptosis in two clinically relevant tumour cell lines (Panc-1 pancreas carcinoma and HT-29 colon carcinoma) and in non-malignant human foreskin fibroblasts. The demethylcantharidin and the bipyridine conjugates retained the cytotoxicity of the parent illudin M while displaying an improved specificity for the tumour cells over the fibroblasts. |
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Authors:
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Rainer Schobert; Bernhard Biersack; Sebastian Knauer; Matthias Ocker |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2008-08-07 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: 16 ISSN: 1464-3391 ISO Abbreviation: Bioorg. Med. Chem. Publication Date: 2008 Sep |
Date Detail:
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Created Date: 2008-09-17 Completed Date: 2008-12-05 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: 8592-7 Citation Subset: IM |
Affiliation:
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Organic Chemistry Laboratory, University of Bayreuth, Universitätsstrasse 30, 95440 Bayreuth, Germany. Rainer.Schobert@uni-bayreuth.de |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Agaricales
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growth & development,
metabolism* Cell Line, Tumor / drug effects Chlorambucil / chemistry, pharmacology Colonic Neoplasms / metabolism, pathology Cytotoxins / chemistry, isolation & purification, pharmacology* Dicarboxylic Acids / chemistry, pharmacology Docosahexaenoic Acids / chemistry, pharmacology Esters / chemistry, pharmacology* Fibroblasts / cytology, drug effects* Humans Pancreatic Neoplasms / metabolism, pathology Sesquiterpenes / chemistry, isolation & purification, pharmacology Structure-Activity Relationship Toxicity Tests |
| Chemical | |
Reg. No./Substance:
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0/Cytotoxins; 0/Dicarboxylic Acids; 0/Esters; 0/Sesquiterpenes; 1146-04-9/illudin M; 145-73-3/endothall; 25167-62-8/Docosahexaenoic Acids; 305-03-3/Chlorambucil |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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