Carboxamide derivatives induce apoptosis in the U251 glioma cell line.

Abstract

Glioma is a malignant tumor that is frequently treated using chemotherapy. The aim of the present study was to examine the antitumor activity of two novel carboxamide derivatives in glioma, and investigate the underlying mechanisms. Two previously designed and synthesized carboxamide derivatives were selected and their effects on glioma cells were evaluated. Specifically, assays to evaluate proliferation, apoptosis, oxidation, caspase-3, -8 and -9 activity, and the expression of Bcl-2 and surviving in glioma cells were conducted. The carboxamide derivatives were revealed to inhibit proliferation, as well as to induce apoptosis and oxidative damage in glioma U251 cells. In addition, the carboxamide derivatives increased the activity of caspase-3, -8 and -9, and suppressed the expression of Bcl-2 and survivin. These findings demonstrate that the carboxamide derivatives displayed antitumor activity against glioma in vitro, which may have been mediated via the induction of oxidative damage and apoptosis.