Synthesis of new indeno[1,2-e] pyrimido[4,5-b][1,4] diazepine-5,11-diones as potential antitumor agents

被引:42
|
作者
Insuasty, Braulio [1 ]
Orozco, Fabian [1 ]
Lizarazo, Carolina [1 ]
Quiroga, Jairo [1 ]
Abonia, Rodrigo [1 ]
Hursthouse, Mike [2 ]
Nogueras, Manuel [3 ]
Cobo, Justo [3 ]
机构
[1] Univ Valle, Dept Chem, Heterocycl Cpds Res Grp, Cali 25360, Colombia
[2] Univ Southampton, Sch Chem, Southampton SO17 1BJ, Hants, England
[3] Univ Jaen, Dept Inorgan & Organ Chem, Jaen 23071, Spain
关键词
regioselective cyclocondensation; 5,6-diamino-3,4-dihydropyrimidin-4-ones; 2-arylideneindandiones; indenopyrimido[4,5-b][1,4] diazepine; antitumoral;
D O I
10.1016/j.bmc.2008.08.023
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Novel racemic indeno[1,2-e] pyrimido[4,5-b][1,4] diazepine-5,11-diones 3 -29 were obtained regioselectivily from the reaction of 5,6-diamino-3,4-dihydropyrimidin-4-ones 1 and 2-arylideneindandiones 2 as reagents. These compounds have been evaluated at the US National Cancer Institute (NCI) for their ability to inhibit approximately 60 different human tumor cell lines, where 5 and 6 presented remarkable activity against 57 and 48 cancer cell lines, respectively, with the most important GI(50) values ranging from 0.49 to 1.46 mu M, in vitro assay. (C) 2008 Published by Elsevier Ltd.
引用
收藏
页码:8492 / 8500
页数:9
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