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

被引:30
|
作者
El-Tombary, Alaa A. [1 ]
Abdel-Ghany, Yasser S. [1 ]
Belal, Ahmad S. F. [1 ]
El-Dine, Shams A. Shams [1 ]
Soliman, Farid S. G. [1 ]
机构
[1] Univ Alexandria, Fac Pharm, Dept Pharmaceut Chem, Alexandria, Egypt
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; CYCLIN-DEPENDENT KINASES; ASCORBIC-ACID ANALOGS; SELECTIVE INHIBITOR; ANTITUMOR AGENTS; ALPHA; CDK2; BIOACTIVITIES; CYTOTOXICITY; ROSCOVITINE; NUCLEOSIDES;
D O I
10.1007/s00044-010-9394-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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-l, 9, 11) and derived halogenated quinoxalin-2(1H)-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.
引用
收藏
页码:865 / 876
页数:12
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