Synthesis of some substituted furan-2(5H)-ones and derived quinoxalinones as potential anti-microbial and anti-cancer agents

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• 作者：Alaa A. El-Tombary (1)
  Yasser S. Abdel-Ghany (1)
  Ahmad S. F. Belal (1)
  Shams A. Shams El-Dine (1)
  Farid S. G. Soliman (1)
  
• 关键词：5 ; Aryl ; 4 ; halo ; 3 ; hydroxyfuran ; 2(5H) ; ones ; 3 ; (2 ; Aryl ; 1 ; halovinyl)quinoxalin ; 2(1H) ; ones ; 3 ; Aryl ; 2 ; bromo ; 2 ; propenoic acids ; Anti ; cancer and anti ; microbial properties
• 刊名：Medicinal Chemistry Research
• 出版年：2011
• 出版时间：September 2011
• 年：2011
• 卷：20
• 期：7
• 页码：865-876
• 全文大小：384KB
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• 作者单位：Alaa A. El-Tombary (1)
  Yasser S. Abdel-Ghany (1)
  Ahmad S. F. Belal (1)
  Shams A. Shams El-Dine (1)
  Farid S. G. Soliman (1)
  
  1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt
  

文摘

In search for novel anti-cancer and anti-microbial agents with promising pharmacotoxicological profile, the synthesis of some substituted 4-halofuran-2(5H)-ones (8a-strong class="a-plus-plus">l, 9, 11) and derived halogenated quinoxalin-2(1H)-ones (12a-strong class="a-plus-plus">d) is described. Some of the halogenated furanones were readily oxidized to the corresponding 2-bromo-2-propenoic acids (13a-strong class="a-plus-plus">c) with hydrogen peroxide in alkaline medium. Twenty-two compounds were preliminary tested for their in vitro activity against three bacteria and one fungus and revealed encouraging activity. On the other hand, three compounds were screened as anti-cancer agents using cell line panel protocol and 22 compounds were subjected to cycline-dependent kinases (CDKs) inhibition screening program but were inactive.