Synthesis and antitumor activity of novel tetrahydro-beta-carboline derivatives as KSP inhibitors / 药学学报
Acta Pharmaceutica Sinica
; (12): 1119-1123, 2013.
Article
in Zh
| WPRIM
| ID: wpr-259506
Responsible library:
WPRO
ABSTRACT
Inhibitors of kinesin spindle protein (KSP) are a promising class of anticancer agents that cause mitotic arrest and induce apoptosis of tumor cells. A series of novel tetrahydro-beta-carboline derivatives were synthesized as kinesin spindle protein inhibitor and evaluated as potential antitumor agents. All compounds showed promising KSP inhibitiory activity. Compounds 8 and 9 exhibited better antitumor activity (Lung/A549, Stomach/AGS) than CK0106023 with GI50/IC50 values (1.07/1.62 and 1.46/3.27 micromol x L(-1), 1.09/>10 and 1.22/6.33 micromol x L(-1), respectively).
Full text:
1
Index:
WPRIM
Main subject:
Pharmacology
/
Carbolines
/
Molecular Structure
/
Chemistry
/
Kinesins
/
Inhibitory Concentration 50
/
Cell Line, Tumor
/
Cell Proliferation
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Antineoplastic Agents
Limits:
Humans
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2013
Type:
Article