Stiz Dorimar, Campos Adriana, Lúcia Tasca Gois Ruiz Ana, Ernesto de Carvalho João, Corrêa Rogério, Cechinel-Filho Valdir
Z Naturforsch C J Biosci. 2016 Nov 1;71(11-12):423-427. doi: 10.1515/znc-2016-0067.
This work describes the antiproliferative potential of 14 cyclic imides (methylphtalimides, carboxylic acid phtalimides and itaconimides) against several human cancer cell lines. The antiproliferative effect was evaluated using the sulforhodamine B assay. Although some compounds from methylphtalimide and carboxylic acid phtalimide classes exhibited a selective antiproliferative activity, the itaconimides (11-14) exhibited the best results, especially compound 14, which presented a TGI (concentration that produces total growth inhibition) value of 0.0043 μM against glioma (U251), being inactive against the non-tumor cell line (HaCat). Absorption, distribution, metabolism and excretion in silico evaluations suggest that these compounds are promising candidates.
这项研究描述了14种环状酰亚胺（甲基邻苯二甲酰亚胺、羧酸邻苯二甲酰亚胺和衣康酰亚胺）对几种人类癌细胞系的抗增殖潜力。使用磺酰罗丹明B测定法评估抗增殖效果。虽然甲基邻苯二甲酰亚胺和羧酸邻苯二甲酰亚胺类的一些化合物表现出选择性抗增殖活性，但衣康酰亚胺（11 - 14）表现出最佳结果，尤其是化合物14，其对胶质瘤（U251）的TGI（产生完全生长抑制的浓度）值为0.0043 μM，对非肿瘤细胞系（HaCat）无活性。计算机模拟的吸收、分布、代谢和排泄评估表明这些化合物是有前景的候选物。
