title: Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors.
abstract: A novel triazole-containing chemical series was shown to inhibit tubulin polymerization and cause cell cycle arrest in A431 cancer cells with EC(50) 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.
authors.affiliation: Department of Chemistry, ImClone Systems, 710 Parkside Avenue, Suite 2, Brooklyn, NY 11226, USA. shawn_ouyang@yahoo.com
authors.forename: Xiaohu
authors.initials: X
authors.lastname: Ouyang
authors.forename: Xiaoling
authors.initials: X
authors.lastname: Chen
authors.forename: Evgueni L
authors.initials: EL
authors.lastname: Piatnitski
authors.forename: Alexander S
authors.initials: AS
authors.lastname: Kiselyov
authors.forename: Hai-Ying
authors.initials: HY
authors.lastname: He
authors.forename: Yunyu
authors.initials: Y
authors.lastname: Mao
authors.forename: Vatee
authors.initials: V
authors.lastname: Pattaropong
authors.forename: Yang
authors.initials: Y
authors.lastname: Yu
authors.forename: Ki H
authors.initials: KH
authors.lastname: Kim
authors.forename: John
authors.initials: J
authors.lastname: Kincaid
authors.forename: Leon
authors.initials: L
authors.lastname: Smith
authors.forename: Wai C
authors.initials: WC
authors.lastname: Wong
authors.forename: Sui Ping
authors.initials: SP
authors.lastname: Lee
authors.forename: Daniel L
authors.initials: DL
authors.lastname: Milligan
authors.forename: Asra
authors.initials: A
authors.lastname: Malikzay
authors.forename: James
authors.initials: J
authors.lastname: Fleming
authors.forename: Jason
authors.initials: J
authors.lastname: Gerlak
authors.forename: Dhanvanthri
authors.initials: D
authors.lastname: Deevi
authors.forename: Jacqueline F
authors.initials: JF
authors.lastname: Doody
authors.forename: Hui-Hsien
authors.initials: HH
authors.lastname: Chiang
authors.forename: Sheetal N
authors.initials: SN
authors.lastname: Patel
authors.forename: Ying
authors.initials: Y
authors.lastname: Wang
authors.forename: Robin L
authors.initials: RL
authors.lastname: Rolser
authors.forename: Paul
authors.initials: P
authors.lastname: Kussie
authors.forename: Marc
authors.initials: M
authors.lastname: Labelle
authors.forename: M Carolina
authors.initials: MC
authors.lastname: Tuma
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008870:Microtubules / Q000187:drug effects; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D050257:Tubulin Modulators / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D014230:Triazoles; D050257:Tubulin Modulators; C045575:1,2,4-triazole