合成环酰亚胺(甲基酞酰亚胺、羧酸酞酰亚胺和伊塔康酰亚胺)对人癌细胞系的抗增殖作用

D. Stiz, Adriana Campos, Ana Lúcia Tasca Gois Ruiz, João Ernesto de Carvalho, R. Corrêa, V. Cechinel-Filho
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引用次数: 4

摘要

摘要:本文描述了14种环亚胺(甲基酞酰亚胺、羧酸酞酰亚胺和伊塔康酰亚胺)对几种人类癌细胞系的抗增殖潜力。采用硫代丹胺B法评价其抗增殖作用。虽然甲基酞酰亚胺类化合物和羧酸酞酰亚胺类化合物具有选择性的抗增殖活性,但伊塔康酰亚胺类化合物(11-14)表现出最好的效果,特别是化合物14,其对胶质瘤(U251)的TGI(产生总生长抑制的浓度)值为0.0043 μM,对非肿瘤细胞系(HaCat)无活性。吸收,分布,代谢和排泄在硅评价表明,这些化合物是有希望的候选者。
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Antiproliferative effect of synthetic cyclic imides (methylphtalimides, carboxylic acid phtalimides and itaconimides) against human cancer cell lines
Abstract 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.
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