Synthesis and biological evaluations of novel pyrazinoic acid derivatives as anticancer agents

Pyrazinoic acid or pyrazine-2-carboxylic (PA), due to its nitrogenous heteroaromatic ring, can be explored as an anticancer agent. Here, a series of twenty novels PA derivatives have been synthesized and characterized using IR, NMR, mass spectrums. Their cytotoxic activity was evaluated against three different cancer cell lines, including lung (A549), breast (MCF-7), colon (HT-29). P16, the most potent compound, showed moderate cytotoxicity with IC50 6.11, 10.64, 14.92 μM, A549, MCF-7, HT-29 respectively. Furthermore, effect this compound MRC5 non-tumoral line, exhibited selectivity index 9.02. The apoptotic induction P16 also performed on A549 line. results that concentration increases (from 3 6 μM), percentage apoptosis from 8.54% 72.4%. Electrophoretic gel mobility shift assays able reactive oxygen species (ROS) induce DNA cleavage in presents H2O2 (1.0 mM) high doses. Molecular docking applied anticipate binding locations Bcl-2 regulator their proposed targets.