title: Design, Synthesis and Biological Evaluation of 1,4-Disubstituted-3,4-dihydroisoquinoline Compounds as New Tubulin Polymerization Inhibitors.
abstract: A series of 1,4-disubstituted-3,4-dihydroisoquinoline derivatives designed as tubulin polymerization inhibitors were synthesized. Their cytotoxic activities against the CEM leukemia cell line were evaluated. Most of them displayed moderate cytotoxic activities, and compounds 21 and 32 showed good activities with IC50 of 4.10 and 0.64 μM, respectively. The most potent compound 32 was further confirmed to be able to inhibit tubulin polymerization, and its hypothetical binding mode with tubulin was obtained by molecular docking.
authors.affiliation: School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. zhanglingdd7120@163.com.
authors.forename: Ling
authors.initials: L
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. ylsong@smmu.edu.cn.
authors.forename: Yunlong
authors.initials: Y
authors.lastname: Song
authors.affiliation: School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. cpuhuangjj@126.com.
authors.forename: Jingjing
authors.initials: J
authors.lastname: Huang
authors.affiliation: School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. nudt_liujia@hotmail.com.
authors.forename: Jia
authors.initials: J
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. natureholic@163.com.
authors.forename: Wenwen
authors.initials: W
authors.lastname: Zhu
authors.affiliation: School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. zhouyoujun@smmu.edu.cn.
authors.forename: Youjun
authors.initials: Y
authors.lastname: Zhou
authors.affiliation: School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. nudt_liujia@hotmail.com.
authors.forename: Jiaguo
authors.initials: J
authors.lastname: Lv
authors.affiliation: School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. canhuizheng@smmu.edu.cn.
authors.forename: Canhui
authors.initials: C
authors.lastname: Zheng
authors.affiliation: School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. zhuju@smmu.edu.cn.
authors.forename: Ju
authors.initials: J
authors.lastname: Zhu
mesh_terms: D045744:Cell Line, Tumor; D006801:Humans; D020128:Inhibitory Concentration 50; D007546:Isoquinolines / Q000737:chemistry*; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: C109852:G 1616; D007546:Isoquinolines; D050257:Tubulin Modulators