【摘 要】
：
A series of 1-methyl-1H-indole-pyrazoline hybrids were designed,synthesized,and biologically evaluated as potential tubulin polymerization inhibitors.Among
【机 构】
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State Key laboratory of Pharmaceutical Biotechnology,Nanjing University,Nanjing 210023(P.R.China)
【出 处】
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第八届国际分子模拟与信息技术应用学术会议
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 μM)and in vitro growth inhibitory activity against a panel of four human cancer cell lines(IC50 values of 0.21-0.31 μM).Further studies confirmed that compound e19 can induce HeLa cell apoptosis,cause cell-cycle arrest in G2/M phase,and disrupt the cellular microtubule network.These studies,along with molecular docking and 3D-QSAR modeling,provide an important basis for further optimization of compound e19 as a potential anticancer agent.
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