Loriga M, Fiore M, Sanna P, Paglietti G
Istituto di Chimica Farmaceutica, Università di Sassari.
Farmaco. 1995 May;50(5):289-301.
Thirty-five quinoxalines bearing a substituted aniline group on position 2 and various substituents on positions 3,6,7 and 8 were prepared in order to evaluate in vitro anticancer activity. Structural elucidation of some isomeric quinoxalinones formed by ring closure of 4-substituted-1,2-diaminobenzenes with dicarbonyl compounds was achieved by comparison with one isomer coming from an unambiguous independent route. Preliminary in vitro screening at NCI showed that many compounds exhibited a moderate to strong growth inhibition activity on various cell lines between 10(-5) and 10(-4) molar concentrations.
为了评估体外抗癌活性，制备了35种在2位带有取代苯胺基团且在3、6、7和8位带有各种取代基的喹喔啉。通过与一条明确独立路线得到的一种异构体进行比较，实现了对由4-取代-1,2-二氨基苯与二羰基化合物闭环形成的一些异构喹喔啉酮的结构解析。美国国立癌症研究所（NCI）的初步体外筛选表明，许多化合物在10⁻⁵至10⁻⁴摩尔浓度之间对各种细胞系表现出中度至强烈的生长抑制活性。
