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Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors
Ouyang X.; Chen X.; Piatnitski E.L.; Kiselyov A.S.; He H.-Y.; Mao Y.; Pattaropong V.; Yu Y.; Kim K.H.; Kincaid J.; Smith II L.; Wong W.C.; Lee S.P.; Milligan D.L.; Malikzay A.; Fleming J.; Gerlak J.; Deevi D.; Doody J.F.; Chiang H.-H.; Patel S.N.; Wang Y.; Rolser R.L.; Kussie P.; Labelle M.; Tuma M.C.
2005-12-01
Source PublicationBioorganic and Medicinal Chemistry Letters
ISSN0960894X
Volume15Issue:23Pages:5154-5159
AbstractA novel triazole-containing chemical series was shown to inhibit tubulin polymerization and cause cell cycle arrest in A431 cancer cells with EC values in the single digit nanomolar range. Binding experiments demonstrated that representative active compounds of this class compete with colchicine for its binding site on tubulin. The syntheses and structure-activity relationship studies for the triazole derivatives are described herein. © 2005 Elsevier Ltd. All rights reserved.
Keyword1,2,4-Triazole Antimitotic Tubulin inhibitor Tubulin polymerization Tumor vasculature Vascular disrupting agent
DOI10.1016/j.bmcl.2005.08.056
URLView the original
Language英語
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Cited Times [WOS]:56   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
AffiliationEli Lilly and Company
Recommended Citation
GB/T 7714
Ouyang X.,Chen X.,Piatnitski E.L.,et al. Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors[J]. Bioorganic and Medicinal Chemistry Letters,2005,15(23):5154-5159.
APA Ouyang X..,Chen X..,Piatnitski E.L..,Kiselyov A.S..,He H.-Y..,...&Tuma M.C..(2005).Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors.Bioorganic and Medicinal Chemistry Letters,15(23),5154-5159.
MLA Ouyang X.,et al."Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors".Bioorganic and Medicinal Chemistry Letters 15.23(2005):5154-5159.
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