The inflammatory response is a common feature of many pathological conditions, and there is urgent necessity for new substances that minimize the harmful effects of inflammation. Chromenes represent a class of compounds with multiple pharmacological actions that have already been described and may be potential candidates for studies of therapeutic action. This study aimed to test novel 4‐aryl‐4H‐chromene‐derived molecules in an in vitro model of inflammation using lipopolysaccharide (LPS)‐induced Raw 264.7 cells. Seven compounds derived from 4‐aryl‐4H‐chromene were tested on Raw 264.7 cells to evaluate their cytotoxic effects. Next, the effect of the selected compounds on the pro‐inflammatory mediators (tumor necrosis factor‐alpha [TNF‐α], monocyte chemoattractant protein‐1 [MCP‐1], interleukin [IL]‐6) and on the anti‐inflammatory mediators (IL‐10 and IL‐13) was analyzed, and finally, the effect of the compounds on macrophage apoptosis and expression of surface receptors (toll‐like receptor 4 [TLR‐4] and mannose) was evaluated. The results of this study demonstrated that changes in the molecular structure of 4‐aryl‐4H‐chromene altered its cytotoxic profile. Therefore, derivatives that showed safe results were selected for further analyses (named compounds: 4–6). In these experiments, the compounds were able to decrease nitric oxide (NO) levels and production of MCP‐1, IL‐6, IL‐10, and IL‐13. Furthermore, these derivatives were effective in reducing macrophage apoptosis and the expression of surface receptors, as TLR‐4/CD284. Moreover, compounds 5 and 6 also were effective in increasing mannose receptor (CD206) expression. The results indicate, for the first time to our knowledge, that the anti‐inflammatory effect produced by chromenes is linked to macrophage repolarization (M1 to M2).
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