Structure-activity relationships study of -ethylene glycol-comprising alkyl heterocyclic carboxamides against A549 lung cancer cells.

Certain cancer cells depend on oxidative phosphorylation for survival; thus, inhibiting this process may be a promising treatment strategy. This study explored the structure-activity relationships of the mitochondrial inhibitor -ethylene glycol-comprising alkyl thiophene-3-carboxamide . We synthesized and evaluated 13 analogs (-) with different ethylene glycol units, heterocycles and connecting groups for their growth-inhibitory effects on A549 non-small cell lung cancer cells. We found that increasing the number of ethylene glycol units significantly enhanced inhibitory activity. Some analogs activated adenosine monophosphate-activated protein kinase, similar to . Notably, analog , which contains tetraethylene glycol units, significantly inhibited tumor growth . Analog may be a potential therapeutic agent for non-small cell lung cancer treatment.