Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines

doi:10.1016/j.bmcl.2005.11.094

Residential College	false
Status	已發表Published
	Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines
	Ouyang X.; Piatnitski E.L.; Pattaropong V.; Chen X.; He H.-Y.; Kiselyov A.S.; Velankar A.; Kawakami J.; Labelle M.; Smith II L.; Lohman J.; Lee S.P.; Malikzay A.; Fleming J.; Gerlak J.; Wang Y.; Rosler R.L.; Zhou K.; Mitelman S.; Camara M.; Surguladze D.; Doody J.F.; Tuma M.C.
	2006-03-01
Source Publication	Bioorganic and Medicinal Chemistry Letters
ISSN	0960894X
Volume	16 Issue:5 Pages:1191-1196
Abstract	Oxadiazole derivatives were synthesized and evaluated for their ability to inhibit tubulin polymerization and to cause mitotic arrest in tumor cells. The most potent compounds inhibited tubulin polymerization at concentrations below 1 μM. Lead analogs caused mitotic arrest of A431 human epidermoid cells and cells derived from multi-drug resistant tumors (10, EC = 7.8 nM). Competition for the colchicine binding site and pharmacokinetic properties of selected potent compounds were also investigated and are reported herein, along with structure-activity relationships for this novel series of antimitotic agents. © 2005 Elsevier Ltd. All rights reserved.
Keyword	1,3,4-oxadiazole Antimitotic Agent Multiple-drug Resistance Tubulin Polymerization Inhibitor
DOI	10.1016/j.bmcl.2005.11.094
URL	View the original
Language	英語English
WOS ID	WOS:000235284700019
Scopus ID	2-s2.0-31344448309
Fulltext Access	View Full-Text via DOI View Full-Text via Web of Science View Full-Text via Scopus
Citation statistics
Document Type	Journal article
Collection	University of Macau
Affiliation	Eli Lilly and Company
Recommended Citation GB/T 7714	Ouyang X.,Piatnitski E.L.,Pattaropong V.,et al. Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines[J]. Bioorganic and Medicinal Chemistry Letters, 2006, 16(5), 1191-1196.
APA	Ouyang X.., Piatnitski E.L.., Pattaropong V.., Chen X.., He H.-Y.., Kiselyov A.S.., Velankar A.., Kawakami J.., Labelle M.., Smith II L.., Lohman J.., Lee S.P.., Malikzay A.., Fleming J.., Gerlak J.., Wang Y.., Rosler R.L.., Zhou K.., Mitelman S.., ...& Tuma M.C. (2006). Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines. Bioorganic and Medicinal Chemistry Letters, 16(5), 1191-1196.
MLA	Ouyang X.,et al."Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines".Bioorganic and Medicinal Chemistry Letters 16.5(2006):1191-1196.

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