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Abstract <p>A series of novel isoxazole functionalized quinazolinone derivatives was prepared by hydrolysis of 2-amino-6-(trifluoromethyl)benzonitrile to 2-amino-6-(trifluoromethyl)benzoic acid, followed by the reaction with phenyl isothiocyanate to get 2-mercapto-3-phenyl-5-(trifluoromethyl)quinazolin-4(3<i>H</i>)-one, which was further alkylated with propargyl bromide to obtain propargylated quinazolinone derivatives. Terminal propargyl group was reacted with various substituted benzaldehyde oximes in the presence of strong base to get isoxazole substituted quinazolinone derivatives. All the final compounds evaluated for anticancer activity against four human cancer cell lines such as HeLa, COLO 205, HepG2, MCF7 and promising compounds were revealed.</p>

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Novel Isoxazole Functionalized Quinazolinone Derivatives and Their Anticancer Activity

  • 期刊论文

  • 发表日期：

    2025年1月1日

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  • S. K. Konda,
  • A. K. Kanuri,
  • B. K. Chennuri,
  • R. Anjum,
  • R. Trivedi,
  • M. Patlola,
  • S. Yamini,
  • S. Bhoomandla

摘要

Abstract

A series of novel isoxazole functionalized quinazolinone derivatives was prepared by hydrolysis of 2-amino-6-(trifluoromethyl)benzonitrile to 2-amino-6-(trifluoromethyl)benzoic acid, followed by the reaction with phenyl isothiocyanate to get 2-mercapto-3-phenyl-5-(trifluoromethyl)quinazolin-4(3H)-one, which was further alkylated with propargyl bromide to obtain propargylated quinazolinone derivatives. Terminal propargyl group was reacted with various substituted benzaldehyde oximes in the presence of strong base to get isoxazole substituted quinazolinone derivatives. All the final compounds evaluated for anticancer activity against four human cancer cell lines such as HeLa, COLO 205, HepG2, MCF7 and promising compounds were revealed.