Conejo-García Ana, Núñez María C, Marchal Juan A, Rodríguez-Serrano Fernando, Aránega Antonia, Gallo Miguel A, Espinosa Antonio, Campos Joaquín M
Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, c/ Campus de Cartuja s/n, 18071 Granada, Spain.
Eur J Med Chem. 2008 Aug;43(8):1742-8. doi: 10.1016/j.ejmech.2007.10.025. Epub 2007 Oct 25.
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.
本文介绍了对(RS)-6-取代-7或9-(2,3-二氢-5H-1,4-苯并二氧杂环庚三烯-3-基)-7H-或-9H-嘌呤的合成及药理评价的扩展研究。微波辅助有机合成能够更快地获得目标化合物,其优点是可以选择性地获得N-7'或N-9'区域异构体,从而简化了它们的分离过程。为了测试产物(包括嘌呤碱)在细胞系统中的行为,测定了对MCF-7人乳腺癌细胞系的细胞毒性活性,并使用三种活性最高的化合物研究了MCF-7细胞系中的细胞周期分布和细胞凋亡情况。