Synthesis and antitumor activity of novel tetrahydro-beta-carboline derivatives as KSP inhibitors.
- Author:
Xiu-Qin RUAN
1
;
Ming CHEN
;
Wu-Tong WU
;
Qi-Dong YOU
Author Information
1. Key Laboratory of Carcinogenesis and Intervention of Jiangsu Province, China Pharmaceutical University, Nanjing 210009, China.
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Carbolines;
chemical synthesis;
chemistry;
pharmacology;
Cell Line, Tumor;
Cell Proliferation;
drug effects;
Humans;
Inhibitory Concentration 50;
Kinesin;
antagonists & inhibitors;
pharmacology;
Molecular Structure
- From:
Acta Pharmaceutica Sinica
2013;48(7):1119-1123
- CountryChina
- Language:Chinese
-
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).
