【摘 要】
:
A series of 1-methyl-1H-indole–pyrazoline hybrids were designed,synthesized,and biologically evaluated as potential tubulin polymerization inhibitors.Among the
【机 构】
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StateKeyLaboratoryofPharmaceuticalBiotechnology,NanjingUniversity,Nanjing210023P.R.China
【出 处】
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第九届国际分子模拟与信息技术应用学术会议(ICMS&I2018)
论文部分内容阅读
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).
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