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Abstract <p>A series of novel <i>N</i>-[5-(trifluoromethyl)-1<i>H</i>-indazol-3-yl]acetamide derivatives were synthesized starting from 2-hydroxy-5-(trifluoromethyl)benzonitrile. The starting compound was reacted with hydrazine hydrate to get 5-(trifluoromethyl)-1<i>H</i>-indazol-3-amine. Further reaction with chloroacetic anhydride to get 2-chloro-<i>N</i>-[5-(trifluoromethyl)-1<i>H</i>-indazol-3-yl]acetamide. This compound reacts with thiophenols or piperazines to afford designed ethyl amide-linked trifluoromethyl indazole hybrids. All the final compounds were evaluated for anticancer activity against four human cancer cell lines such as: HeLa-Cervical cancer (CCL-2), COLO 205-Colon cancer (CCL-222), HepG2-Liver cancer (HB-8065), MCF7-Breast cancer (HTB-22), and one normal cell line such as HEK-293 Human Embryonic Kidney cells (CRL-1573) and promising compounds have been identified. Molecular docking interactions were also evaluated.</p>

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Construction of N-[5-(Trifluoromethyl)-1H-indazol-3-yl]acetamide Derivatives; Their Anticancer Activity and Molecular Docking Interactions

  • 期刊论文

  • 发表日期：

    2025年12月1日

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  • Boya Venkata Swamy,
  • Rashmi Trivedi,
  • Ganji Sreekanth Reddy,
  • Gundu Mallikarjun,
  • Rumandla Lavanya,
  • Amrita Saha,
  • Mendam Kishore,
  • Banothu Devendar,
  • Bhoomandla Srinu

摘要

Abstract

A series of novel N-[5-(trifluoromethyl)-1H-indazol-3-yl]acetamide derivatives were synthesized starting from 2-hydroxy-5-(trifluoromethyl)benzonitrile. The starting compound was reacted with hydrazine hydrate to get 5-(trifluoromethyl)-1H-indazol-3-amine. Further reaction with chloroacetic anhydride to get 2-chloro-N-[5-(trifluoromethyl)-1H-indazol-3-yl]acetamide. This compound reacts with thiophenols or piperazines to afford designed ethyl amide-linked trifluoromethyl indazole hybrids. All the final compounds were evaluated for anticancer activity against four human cancer cell lines such as: HeLa-Cervical cancer (CCL-2), COLO 205-Colon cancer (CCL-222), HepG2-Liver cancer (HB-8065), MCF7-Breast cancer (HTB-22), and one normal cell line such as HEK-293 Human Embryonic Kidney cells (CRL-1573) and promising compounds have been identified. Molecular docking interactions were also evaluated.