title: [Synthesis and antitumor activity of novel tetrahydro-beta-carboline derivatives as KSP inhibitors].
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).
authors.affiliation: Key Laboratory of Carcinogenesis and Intervention of Jiangsu Province, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Xiu-Qin
authors.initials: XQ
authors.lastname: Ruan
authors.forename: Ming
authors.initials: M
authors.lastname: Chen
authors.forename: Wu-Tong
authors.initials: WT
authors.lastname: Wu
authors.forename: Qi-Dong
authors.initials: QD
authors.lastname: You
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002243:Carbolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D016547:Kinesins / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D015394:Molecular Structure
chemical_list: D000970:Antineoplastic Agents; D002243:Carbolines; C470243:KIF11 protein, human; C009804:tryptoline; D016547:Kinesins