Loriga M, Piras S, Sanna P, Paglietti G
Istituto di Chimica Farmaceutica, Università di Sassari.
Farmaco. 1997 Mar;52(3):157-66.
Thirty-three quinoxalines bearing an aminobenzoyl or aminobenzoylglutamate group on position 2 and various substituents on position 3,6,7 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI 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(-6) M. Among the series examined one compound (29) which was the most active also exhibited both in vitro anti-HIV protection and antifungal activity while in other two (31, 37) the antifungal activity was prevailing.
为了评估体外抗癌活性，制备了33种在喹喔啉的2位带有氨基苯甲酰基或氨基苯甲酰基谷氨酸基团且在杂环的3、6、7位带有各种取代基的喹喔啉。美国国立癌症研究所（NCI）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10⁻⁶摩尔之间也记录到了有趣的选择性。在所研究的系列中，活性最强的一种化合物（29）还表现出体外抗HIV保护和抗真菌活性，而另外两种化合物（31、37）则以抗真菌活性为主。
