CAS 143782-20-1: 4-(4,4-Dimethyl-2,5-dioxo-1-imidazolidinyl)-2-(trifluoromethyl)benzonitrile

4-trifluoromethyl-2,5-dioxoimidazolidin-1-yl)benzonitrile is a potent and selective inhibitor of the enzyme histone deacetylase. It binds to the active site of HDACs and inhibits their activity. This inhibition leads to a paradigm shift in the mechanism of HDACs, which blocks the transcription of genes that regulate cell proliferation. 4-(4,4-Dimethyl-2,5-dioxoimidazolidin-1-yl)-2-trifluoromethylbenzonitrile also has cytotoxic effects on prostate cancer cells. This drug is designed as an anticancer agent for use in cancer therapy.

Applications 4-(4,4-Dimethyl-2,5-dioxo-1-imidazolidinyl)-2-(trifluoromethyl)benzonitrile is an intermediate in the synthesis of Oxo-MDV 3100 (Oxo-enzalutamide) (O857800), which is an impurity of Enzalutamide (M199800), which is an androgen-receptor antagonist that blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. Enzalutamide has been shown to induce tumor cell apoptosis, and is used for the treatment of castration-resistant prostate cancer. References Scher, H.I. et al.: Lancet, 375, 1437 (2010); Bellmunt, J. et al.: Ther. Adv. Med. Oncol., 2, 189 (2010); Ryan, C.J. et al.: J. Clin. Oncol., 29, 3651 (2011); Ma, X., et al.: J. Pharm. Biomed. Anal., 131, 436 (2016);