Design, Synthesis and Bio-evaluations of Tetrahydroisoquinolines as Novel Kinesin Spindle Protein (KSP) Inhibitors

摘要：

Based on the pharmacophore we have mapped and the binding structure of monastrol with the target protein，a series of tetrahydroisoquinolines have been identified as novel kinesin spindle protein(KSP)inhibitors. Human KSP protein was cloned，expressed and purified; KSP inhibitory activities of the designed compounds were tested. All the designed compounds displayed more potent inhibitory activities in the KSP ATPase assays and about half of them showed better in vitro cytotoxicities against HepG2 cell line，the first reported small molecule KSP inhibitor monastrol was used as a control compound.

关键词： 蛋白抑制剂 生物评价 合成路线 药物设计

作者: Cheng Jiang Qidong You Lei Yang Mengling Chen Fei Liu Wutong Wu Jiwang Chern

作者单位: Department of Medicinal Chemistry,China Pharmaceutical University, 24 Tongjiaxiang,Nanjing 210009, C School of Life Science and Technology, China Pharmaceutical University, 24 Tongjiaxiang,Nanjing 2100 School of Pharmacy, College of Medicine, National Taiwan University, No. 1, Section 1, Jen-Ai Road,

会议类型: 国内会议

会议名称: 2008中国药学会学术年会暨第八届中国药师周

会议地点: 石家庄

会议语种:英文

页码: 1-9

在线出版日期: 2008-10-18（万方平台首次上网日期，不代表论文的发表时间）