Loriga M, Moro P, Sanna P, Paglietti G, Zanetti S
Istituto di Chimica Farmaceutica, Università di Sassari.
Farmaco. 1997 Aug-Sep;52(8-9):531-7.
Thirty quinoxalines bearing a substituted anilino group on position 2, a carboethoxy or carboxy group on position 3 and a trifluoromethyl group on position 6 or 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 for a few compounds. One single compound exhibited good activity against Candida albicans.
为了评估体外抗癌活性，制备了30种喹喔啉类化合物，这些化合物在杂环的2位带有取代苯胺基，3位带有乙氧羰基或羧基，6位或7位带有三氟甲基。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 M之间，少数化合物也表现出有趣的选择性。有一种化合物对白色念珠菌表现出良好的活性。
