Synthesis and antiproliferative properties of N_3/8-disubstituted 3,8-diazabicyclo[3.2.1]octane analogues of 3,8-bis[2-(3,4,5-trimethoxyphenyl)pyridin-4-yl]methyl-piperazine

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• 作者：Rosanna Filosa ; Antonella Peduto ; Paolo de Caprariis ; Carmela Saturnino ; Michela Festa ; Antonello Petrella ; Amedeo Pau ; Gé ; rard Aimé ; Pinna ; Paolo La Colla ; Bernardetta Busonera ; Roberta Loddo
• 关键词：Piperazine ; 3 ; 8-Diazabicyclo[3.2.1]octane
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2007
• 出版时间：March 2007
• 年：2007
• 卷：42
• 期：3
• 页码：293-306
• 全文大小：488 K

文摘

A series of novel N_3/8-disubstituted-3,8-diazabicyclo[3.2.1]octanes in order to improve the in vitro activity of the prototype 3,8-bis[2-(3,4,5-trimethoxyphenyl)pyridyl-4-yl)methylpiperazine (1) were synthesized and evaluated by assays of growth inhibition against several tumor cell lines. Compounds 2a,b,f and m demonstrated not only growth-inhibitory activities against leukemia cancer cells, but also fairly good activities against the growth of certain solid tumors. Among them, 2a is the most potent one with IC₅₀ values in the low micromolar range. Moreover, compound 2a has been selected for in vitro testing on MCF-7 cell to evaluate the mode of action of this lead compound.