Regiospecific microwave-assisted synthesis and cytotoxic activity against human breast cancer cells of (RS)-6-substituted-7-or 9-(2,3-dihydro-5H-1,4-benzodioxepin-3-yl)-7H- or-9H-purines

被引:22
作者
Conejo-Garcia, Ana [1 ]
Nunez, Maria C. [1 ]
Marchal, Juan A. [2 ]
Rodriguez-Serrano, Fernando [3 ]
Aranega, Antonia [2 ]
Gallo, Miguel A. [1 ]
Espinosa, Antonio [1 ]
Campos, Joaquin M. [1 ]
机构
[1] Fac Farm, Dept Quim Farmaceut & Organ, Granada 18071, Spain
[2] Fac Med, Dept Anat & Embryol Humana, Granada 18071, Spain
[3] Fac Ciencias Expt, Dept Ciencias Salud, Jaen 23071, Spain
关键词
antitumour compounds; seven-membered rings; microwave; MCF-7; 6-substituted purines;
D O I
10.1016/j.ejmech.2007.10.025
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Extended studies on the synthesis and pharmacological evaluation of (RS)-6-substituted-7 or 9-(2,3-dihydro-5H-1,4-benzodioxepin-3-yl)-7H- or -9H-purines are presented. The microwave-assisted organic synthesis has provided faster access to the target compounds with the advantage of selective obtaining the N-7 ' or N-9 ' regioisomers simplifying their isolation. To test the behaviour of the products (including the purine bases) on cellular systems, cytotoxic activity against the MCF-7 human breast cancer cell line was determined, and the three most active compounds were used to study the cell cycle distribution and apoptosis in the MCF-7 cell line. (c) 2007 Elsevier Masson SAS. All fights reserved.
引用
收藏
页码:1742 / 1748
页数:7
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