title: Microtubule inhibitory effects of various SJ compounds on tissue culture cells.
abstract: SJ compounds (SJ8002 and related compounds) are a group of novel anticancer agents (Cho, Chung, Lee, Kwon, Kang, Joo, and Oh. PCT/KR02/00392). To explore the anticancer mechanism of these compounds, we examined the effect of SJ8002 on microtubules of six human cell lines. At a high concentration (2 microg/mL), SJ8002 effectively disrupted microtubules of the six cell lines within 1 h. At lower concentrations (0.05 to approximately 1.0 microg/mL), the antimicrotubule activity of SJ8002 varied defending on cell lines. The inhibition of in vitro polymerization of pure tubulin by SJ8002 suggested that SJ8002 acts on free tubulin, inhibits the polymerization of tubulin dimer into microtubules, and hence induces the depolymerization of microtubules.
authors.affiliation: Department of Biology and the Institute of Life Sciences and Biotechnology, Yonsei University, Seoul 120-749, Korea.
authors.forename: Jong Han
authors.initials: JH
authors.lastname: Lee
authors.forename: Dong Wook
authors.initials: DW
authors.lastname: Kang
authors.forename: Ho Suk
authors.initials: HS
authors.lastname: Kwon
authors.forename: Sun Hwan
authors.initials: SH
authors.lastname: Lee
authors.forename: Si Kyung
authors.initials: SK
authors.lastname: Park
authors.forename: Sun Gan
authors.initials: SG
authors.lastname: Chung
authors.forename: Eui Hwan
authors.initials: EH
authors.lastname: Cho
authors.forename: Soon Young
authors.initials: SY
authors.lastname: Paik
authors.forename: Joo Hun
authors.initials: JH
authors.lastname: Lee
mesh_terms: D000166:Acridines / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D045744:Cell Line, Tumor; D006367:HeLa Cells; D006801:Humans; D008868:Microtubule Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism*; D008870:Microtubules / Q000187:drug effects* / Q000378:metabolism*; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C483162:4-(3,5-dimethylphenyl)piperazine-1-carboxylic acid(5-(1-(3-(acridine-9-yl-amino)-5-hydroxymethylphenylcarbamoyl)-ethylcarbamoyl)-6-ethyl-2-methoxypyridine-3-yl)amide; D000166:Acridines; D000970:Antineoplastic Agents; D008868:Microtubule Proteins; D010879:Piperazines; D011725:Pyridines