Antiproliferative effect of synthetic cyclic imides (methylphtalimides, carboxylic acid phtalimides and itaconimides) against human cancer cell lines

作者：Stiz Dorimar; Campos Adriana; Tasca Gois Ruiz Ana Lucia; de Carvalho Joao Ernesto; Correa Rogerio; Cechinel Filho Valdir

来源：Zeitschrift fur Naturforschung Section C-A Journal of Biosciences, 2016, 71(11-12): 423-427.

DOI：10.1515/znc-2016-0067

• ADME
• antiproliferative effect
• cyclic imides
• itaconimides

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 mu M 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.

• 出版日期2016-11