UM
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 PublicationBioorganic and Medicinal Chemistry Letters
ISSN0960894X
Volume16Issue:5Pages:1191-1196
AbstractOxadiazole 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.
Keyword1,3,4-Oxadiazole Antimitotic agent Multiple-drug resistance Tubulin polymerization inhibitor
DOI10.1016/j.bmcl.2005.11.094
URLView the original
Language英語
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Cited Times [WOS]:74   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
AffiliationEli 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..,...&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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