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

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• 作者：Ana Conejo-Garc&#xed ; a ; Mar&#xed ; a C. Nú ; ñ ; ez ; Juan A. Marchal ; Fern ; o Rodr&#xed ; guez-Serrano ; Antonia Ará ; nega ; Miguel A. Gallo ; Antonio Espinosa ; Joaqu&#xed ; n M. Campos
• 关键词：Antitumour compounds ; Seven-membered rings ; Microwave ; MCF-7 ; 6-Substituted purines
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：August 2008
• 年：2008
• 卷：43
• 期：8
• 页码：1742-1748
• 全文大小：236 K

文摘

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.