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

Medicinal Chemistry Research(2010)

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Abstract
In search for novel anti-cancer and anti-microbial agents with promising pharmacotoxicological profile, the synthesis of some substituted 4-halofuran-2(5 H )-ones ( 8a – l , 9 , 11 ) and derived halogenated quinoxalin-2(1 H )-ones ( 12a – d ) is described. Some of the halogenated furanones were readily oxidized to the corresponding 2-bromo-2-propenoic acids ( 13a – 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.
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Key words
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
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