Discovering a new analogue of thalidomide which may be used as a potent modulator of TNF-α production

A new series of imide derivatives related to thalidomide were synthesized and evaluated as modulators of TNF-α production. These derivatives enhance TNF-α production using human leukemia HL-60 cells induced with 12-O-tetradecanoylphorbol 13-acetate (TPA), while inhibiting TNF-α production induced with okadaic acid (OA) in the same cell line. The diphenylmaleimide derivative 2f, was found to be the most active product, producing a strong modulation of the cytokine level.

Graphical abstractA new series of imide derivatives related to thalidomide were synthesized and evaluated as modulators of TNF-α production. 2f, was found to be the most active product.Figure optionsDownload full-size imageDownload as PowerPoint slide