Loriga M, Fiore M, Sanna P, Paglietti G
Istituto di Chimica Farmaceutica, Università di Sassari.
Farmaco. 1996 Aug-Sep;51(8-9):559-68.
Thirty-one quinoxalines bearing a substituted benzylamino group on position 2 and various substituents on position 3,6,7 and 8 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI on twenty-two compounds showed that most derivatives exhibited a moderate to strong growth inhibition activity on various tumor panel cell lines between 10(-5) and 10(-4) molar concentrations. Interesting selectivities were also recorded between 10(-8) and 10(-5) M.
为了评估体外抗癌活性，制备了31种在喹喔啉的2位带有取代苄氨基且在杂环的3、6、7和8位带有各种取代基的喹喔啉。美国国立癌症研究所（NCI）对22种化合物进行的初步筛选表明，大多数衍生物在10⁻⁵至10⁻⁴摩尔浓度之间对各种肿瘤细胞系表现出中度至强烈的生长抑制活性。在10⁻⁸至10⁻⁵ M之间也记录到了有趣的选择性。
