The present results integrate the previously observed inhibitory profile of the tested compounds against another MAPEG member, i. e., microsomal prostaglandin E2 synthase (mPGES)‐1, suggesting that the 2,4‐dinitro‐biphenyl scaffold is a suitable molecular platform for a multitargeting approach to modulate pro‐inflammatory mediators in inflammation and cancer treatment. Here, PTGES is linked to cancer.