Microtubule inhibitory effects of various SJ compounds on tissue culture cells.
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.
Lee
Jong Han
JH
Department of Biology and the Institute of Life Sciences and Biotechnology, Yonsei University, Seoul 120-749, Korea.
Kang
Dong Wook
DW
Kwon
Ho Suk
HS
Lee
Sun Hwan
SH
Park
Si Kyung
SK
Chung
Sun Gan
SG
Cho
Eui Hwan
EH
Paik
Soon Young
SY
Lee
Joo Hun
JH
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*
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