Cytotoxic and antivascular 1-methyl-4-(3-fluoro-4-methoxyphenyl)-5-(halophenyl)-imidazoles.

2.50
Hdl Handle:
http://hdl.handle.net/10033/364260
Title:
Cytotoxic and antivascular 1-methyl-4-(3-fluoro-4-methoxyphenyl)-5-(halophenyl)-imidazoles.
Authors:
Biersack, Bernhard; Muthukumar, Yazh; Schobert, Rainer; Sasse, Florenz
Abstract:
A series of 1-methyl-4,5-diphenylimidazoles 6 with various patterns of m-halogen substitution at the 5-phenyl ring were tested for cytotoxicity in cancer and nonmalignant cell lines and for their capacity to prevent tube formation in HUVEC cultures. Unlike the monofluoro and difluoro derivatives 6a and 6e, the monobromo and diiodo analogs 6c and 6h were strongly cytotoxic and inhibited the polymerization of tubulin and the tube formation by HUVEC. The dibromo derivative 6g displayed a unique selectivity for KB-3-1 cervix and PC-3 prostate cancer cells. It also inhibited the tube formation by HUVEC and the polymerization of tubulin which is indicative of its potential antiangiogenic activity in solid tumors.
Citation:
Cytotoxic and antivascular 1-methyl-4-(3-fluoro-4-methoxyphenyl)-5-(halophenyl)-imidazoles. 2011, 21 (21):6270-3 Bioorg. Med. Chem. Lett.
Journal:
Bioorganic & medicinal chemistry letters
Issue Date:
1-Nov-2011
URI:
http://hdl.handle.net/10033/364260
DOI:
10.1016/j.bmcl.2011.09.005
PubMed ID:
21963303
Type:
Article
Language:
en
ISSN:
1464-3405
Appears in Collections:
Publications of the research group Chemical Biology (CBIO)

Full metadata record

DC FieldValue Language
dc.contributor.authorBiersack, Bernharden
dc.contributor.authorMuthukumar, Yazhen
dc.contributor.authorSchobert, Raineren
dc.contributor.authorSasse, Florenzen
dc.date.accessioned2015-04-09T11:20:36Zen
dc.date.available2015-04-09T11:20:36Zen
dc.date.issued2011-11-01en
dc.identifier.citationCytotoxic and antivascular 1-methyl-4-(3-fluoro-4-methoxyphenyl)-5-(halophenyl)-imidazoles. 2011, 21 (21):6270-3 Bioorg. Med. Chem. Lett.en
dc.identifier.issn1464-3405en
dc.identifier.pmid21963303en
dc.identifier.doi10.1016/j.bmcl.2011.09.005en
dc.identifier.urihttp://hdl.handle.net/10033/364260en
dc.description.abstractA series of 1-methyl-4,5-diphenylimidazoles 6 with various patterns of m-halogen substitution at the 5-phenyl ring were tested for cytotoxicity in cancer and nonmalignant cell lines and for their capacity to prevent tube formation in HUVEC cultures. Unlike the monofluoro and difluoro derivatives 6a and 6e, the monobromo and diiodo analogs 6c and 6h were strongly cytotoxic and inhibited the polymerization of tubulin and the tube formation by HUVEC. The dibromo derivative 6g displayed a unique selectivity for KB-3-1 cervix and PC-3 prostate cancer cells. It also inhibited the tube formation by HUVEC and the polymerization of tubulin which is indicative of its potential antiangiogenic activity in solid tumors.en
dc.language.isoenen
dc.subject.meshAngiogenesis Inhibitorsen
dc.subject.meshAntineoplastic Agentsen
dc.subject.meshCell Line, Tumoren
dc.subject.meshCells, Cultureden
dc.subject.meshDrug Screening Assays, Antitumoren
dc.subject.meshEndothelium, Vascularen
dc.subject.meshHumansen
dc.subject.meshImidazolesen
dc.titleCytotoxic and antivascular 1-methyl-4-(3-fluoro-4-methoxyphenyl)-5-(halophenyl)-imidazoles.en
dc.typeArticleen
dc.identifier.journalBioorganic & medicinal chemistry lettersen

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