Synthesis and antiproliferative properties of N3/8-disubstituted 3,8-diazabicyclo[3.2.1]octane analogues of 3,8-bis[2-(3,4,5-trimethoxyphenyl)pyridin-4-yl]methyl-piperazine
作者:Rosanna Filosa、Antonella Peduto、Paolo de Caprariis、Carmela Saturnino、Michela Festa、Antonello Petrella、Amedeo Pau、Gérard Aimé Pinna、Paolo La Colla、Bernardetta Busonera、Roberta Loddo
DOI:10.1016/j.ejmech.2006.11.013
日期:2007.3
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
一系列新颖的N(3/8)-双取代-3,8-二氮杂双环[3.2.1]辛烷,以提高原型3,8-bis [2-(3,4,5-)的体外活性合成了三甲氧基苯基)吡啶基-4-基)甲基哌嗪(1),并通过对几种肿瘤细胞系的生长抑制试验进行了评估。化合物2a,b,f和m不仅显示出对白血病癌细胞的生长抑制活性,而且还显示出了对某些实体瘤生长的相当好的活性。其中2a是最有效的,其IC(50)值在低微摩尔范围内。此外,已选择化合物2a在MCF-7细胞上进行体外测试,以评估该先导化合物的作用方式。