Synthesis and Biological Evaluation of 1-Methyl-1H-indole-Pyrazoline Hybrids as Potential Tubulin Polymerization Inhibitors

摘要：

A series of 1-methyl-1H-indole–pyrazoline hybrids were designed,synthesized,and biologically evaluated as potential tubulin polymerization inhibitors.Among them,compound e19 ”5-(5-bromo-1-methyl-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)- 4,5-dihydro-1H-pyrazole-1-carboxamide” showed the most potent inhibitory effect on tubulin assembly (IC50=2.12 mm) and in vitro growth inhibitory activity against a panel of four human cancer cell lines (IC50 values of 0.21–0.31 mm).

关键词： apoptosis indole-pyrazolines inhibitors molecular docking tubulin

作者: Ya-Liang Zhang Ya-Juan Qin Dan-Jie Tang Meng-Ru Yang Bo-Yan Li Yan-Ting Wang Hong-Yu Cai Bao-Zhong Wang Hai-Liang Zhu

作者单位: State Key Laboratory of Pharmaceutical Biotechnology,Nanjing University,Nanjing 210023 P.R.China

会议类型: 国内会议

会议名称: 第九届国际分子模拟与信息技术应用学术会议(ICMS&I2018)

会议地点: 太原

会议语种:英文

页码: 456-469

在线出版日期: 2018-05-01（万方平台首次上网日期，不代表论文的发表时间）