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• W4312469959 endingPage "121" @default.
• W4312469959 startingPage "113" @default.
• W4312469959 abstract "Based on the inhibitory effect of CA-4 analogues and indoles on tubulin polymerization, we designed and synthesized a series of N-((1-methyl-1H-indol-3-yl)methyl)-2-(1H-pyrazol-1-yl or triazolyl)-N-(3,4,5-trimethoxyphenyl)acetamides. All the synthesized compounds were evaluated for their in vitro antiproliferative activities against HeLa, MCF-7 and HT-29 cancer cell lines, and some of the target compounds demonstrated effective activities towards the three tumour cell lines. Among them, compound 7d exhibited the most potent activities against HeLa (IC50 = 0.52 μM), MCF-7 (IC50 = 0.34 μM) and HT-29 (IC50 = 0.86 μM). Mechanistic studies revealed that compound 7d induced cell apoptosis in a dose-dependent manner, arrested the cells in the G2/M phase and inhibited polymerization of tubulin via a consistent way with colchicine. Therefore, 7d is a potential agent for the further development of tubulin polymerization inhibitors." @default.
• W4312469959 created "2023-01-04" @default.
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• W4312469959 date "2023-01-01" @default.
• W4312469959 modified "2023-09-30" @default.
• W4312469959 title "Synthesis and bioactive evaluation of <i>N</i>-((1-methyl-1<i>H</i>-indol-3-yl)methyl)-<i>N</i>-(3,4,5-trimethoxyphenyl)acetamide derivatives as agents for inhibiting tubulin polymerization" @default.
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• W4312469959 doi "https://doi.org/10.1039/d2md00340f" @default.
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