Abstract <p>A novel series of 1,2,3-triazole-quinazoline-acetamide hybrids was synthesized and evaluated for anticancer activity against two breast cancer cell lines, MCF-7 and MDA-MB-231, using erlotinib as a standard drug. The results indicate that 2-[4-(4-methoxyphenyl)-1<i>H</i>-1,2,3-triazol-1-yl]-<i>N</i>-(quinazolin-4-yl)acetamide, 2-[4-(3,5-dimethoxyphenyl)-1<i>H</i>-1,2,3-triazol-1-yl]-<i>N</i>-(quinazolin-4-yl)acetamide, 2-[4-(3-methoxyphenyl)-1<i>H</i>-1,2,3-triazol-1-yl]-<i>N</i>-(quinazolin-4-yl)acetamide, and 2-[4-(4-cyanophenyl)-1<i>H</i>-1,2,3-triazol-1-yl]-<i>N</i>-(quinazolin-4-yl)acetamide exhibited higher activity compared to the standard drug. Additionally, the tyrosine kinase inhibitory activity of 2-[4-(4-methoxyphenyl)-1<i>H</i>-1,2,3-triazol-1-yl]-<i>N</i>-(quinazolin-4-yl)acetamide, 2-[4-(3,5-dimethoxyphenyl)-1<i>H</i>-1,2,3-triazol-1-yl]-<i>N</i>-(quinazolin-4-yl)acetamide, and 2-[4-(3-methoxyphenyl)-1<i>H</i>-1,2,3-triazol-1-yl]-<i>N</i>-(quinazolin-4-yl) acetamide was higher compared to erlotinib.</p>

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Design and Synthesis of 1,2,3-Triazole-quinazoline-acetamide Hybrids; Evaluation of Anticancer Activity and ADMET Analysis

  • Devula Venkata Nagarajesh,
  • Dasari Gouthami,
  • Kandala Satyanarayana,
  • Bandari Srinivas

摘要

Abstract

A novel series of 1,2,3-triazole-quinazoline-acetamide hybrids was synthesized and evaluated for anticancer activity against two breast cancer cell lines, MCF-7 and MDA-MB-231, using erlotinib as a standard drug. The results indicate that 2-[4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl]-N-(quinazolin-4-yl)acetamide, 2-[4-(3,5-dimethoxyphenyl)-1H-1,2,3-triazol-1-yl]-N-(quinazolin-4-yl)acetamide, 2-[4-(3-methoxyphenyl)-1H-1,2,3-triazol-1-yl]-N-(quinazolin-4-yl)acetamide, and 2-[4-(4-cyanophenyl)-1H-1,2,3-triazol-1-yl]-N-(quinazolin-4-yl)acetamide exhibited higher activity compared to the standard drug. Additionally, the tyrosine kinase inhibitory activity of 2-[4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl]-N-(quinazolin-4-yl)acetamide, 2-[4-(3,5-dimethoxyphenyl)-1H-1,2,3-triazol-1-yl]-N-(quinazolin-4-yl)acetamide, and 2-[4-(3-methoxyphenyl)-1H-1,2,3-triazol-1-yl]-N-(quinazolin-4-yl) acetamide was higher compared to erlotinib.