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

Biersack, Bernhard; Muthukumar, Yazh; Schobert, Rainer; Sasse, Florenz

dc.contributor.author	Biersack, Bernhard
dc.contributor.author	Muthukumar, Yazh
dc.contributor.author	Schobert, Rainer
dc.contributor.author	Sasse, Florenz
dc.date.accessioned	2015-04-09T11:20:36Z	en
dc.date.available	2015-04-09T11:20:36Z	en
dc.date.issued	2011-11-01	en
dc.identifier.citation	Cytotoxic and antivascular 1-methyl-4-(3-fluoro-4-methoxyphenyl)-5-(halophenyl)-imidazoles. 2011, 21 (21):6270-3 Bioorg. Med. Chem. Lett.	en
dc.identifier.issn	1464-3405	en
dc.identifier.pmid	21963303	en
dc.identifier.doi	10.1016/j.bmcl.2011.09.005	en
dc.identifier.uri	http://hdl.handle.net/10033/364260	en
dc.description.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.
dc.language.iso	en	en
dc.subject.mesh	Angiogenesis Inhibitors	en
dc.subject.mesh	Antineoplastic Agents	en
dc.subject.mesh	Cell Line, Tumor	en
dc.subject.mesh	Cells, Cultured	en
dc.subject.mesh	Drug Screening Assays, Antitumor	en
dc.subject.mesh	Endothelium, Vascular	en
dc.subject.mesh	Humans	en
dc.subject.mesh	Imidazoles	en
dc.title	Cytotoxic and antivascular 1-methyl-4-(3-fluoro-4-methoxyphenyl)-5-(halophenyl)-imidazoles.	en
dc.type	Article	en
dc.identifier.journal	Bioorganic & medicinal chemistry letters	en
refterms.dateFOA	2018-06-13T03:58:26Z
html.description.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.