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Abstract <p>A series of piperazine-pyrazolo-quinoxalin-2(1<i>H</i>)-one conjugate was synthesized and evaluated for their anticancer activity against two human breast cancer cell lines, such as MCF-7 and MDA-MB231 using erlotinib as a reference drug. The activity results showed that 1-{[3-(4-methoxyphenyl)-1<i>H</i>-pyrazol-5-yl]methyl}-3-(4-methylpiperazin-1-yl)quinoxalin-2(1<i>H</i>)-one, 1-{[3-(3,5-dimethoxyphenyl)-1<i>H</i>-pyrazol-5-yl]methyl}-3-(4-methylpiperazin-1-yl)quinoxalin-2(1<i>H</i>)-one and 1-{[3-(3-methoxyphenyl)-1<i>H</i>-pyrazol-5-yl]methyl}-3-(4-methylpiperazin-1-yl)quinoxalin-2(1<i>H</i>)-one exhibited higher activity as compared to standard drug. The tyrosine kinase EGFR inhibitory activity showed that 1-{[3-(4-methoxyphenyl)-1<i>H</i>-pyrazol-5-yl]methyl}-3-(4-methylpiperazin-1-yl)quinoxalin-2(1<i>H</i>)-one and 1-{[3-(3,5-dimethoxyphenyl)-1<i>H</i>-pyrazol-5-yl]methyl}-3-(4-methylpiperazin-1-yl)quinoxalin-2(1<i>H</i>)-one have higher inhibitory activity as compared to the standard drug erlotinib. Additionally, we performed in silico ADMET for the potent compounds. All the three compounds followed four filters (Lipinski rule, Ghose rule, Veber rule, Egan rule, and Muegge rule) that matched all four of the above-mentioned conditions, except Ghose rule.</p>

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Design, Synthesis, In Vitro Anticancer and ADMET Studies of Piperazine-Pyrazolo-Quinoxalin-2(1H)-one Conjugate as EGFR Targeting Agents

  • 期刊论文

  • 发表日期：

    2025年1月1日

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  • M. Ferazoddin,
  • Arshiya Banu Syeda,
  • Asra Banu Syeda,
  • G. Dasari,
  • S. Bandari

摘要

Abstract

A series of piperazine-pyrazolo-quinoxalin-2(1H)-one conjugate was synthesized and evaluated for their anticancer activity against two human breast cancer cell lines, such as MCF-7 and MDA-MB231 using erlotinib as a reference drug. The activity results showed that 1-{[3-(4-methoxyphenyl)-1H-pyrazol-5-yl]methyl}-3-(4-methylpiperazin-1-yl)quinoxalin-2(1H)-one, 1-{[3-(3,5-dimethoxyphenyl)-1H-pyrazol-5-yl]methyl}-3-(4-methylpiperazin-1-yl)quinoxalin-2(1H)-one and 1-{[3-(3-methoxyphenyl)-1H-pyrazol-5-yl]methyl}-3-(4-methylpiperazin-1-yl)quinoxalin-2(1H)-one exhibited higher activity as compared to standard drug. The tyrosine kinase EGFR inhibitory activity showed that 1-{[3-(4-methoxyphenyl)-1H-pyrazol-5-yl]methyl}-3-(4-methylpiperazin-1-yl)quinoxalin-2(1H)-one and 1-{[3-(3,5-dimethoxyphenyl)-1H-pyrazol-5-yl]methyl}-3-(4-methylpiperazin-1-yl)quinoxalin-2(1H)-one have higher inhibitory activity as compared to the standard drug erlotinib. Additionally, we performed in silico ADMET for the potent compounds. All the three compounds followed four filters (Lipinski rule, Ghose rule, Veber rule, Egan rule, and Muegge rule) that matched all four of the above-mentioned conditions, except Ghose rule.