Synthesis of 21,21-Difluoro-3β-hydroxy-20-methylpregna-5,20-diene and 5,16,20-Triene as potential inhibitors of steroid C17(20) lyase

An efficient dehyrohalogenation method for the synthesis of α,β,β-trifluorostyrenes, α-chloro-β,β-difluorostyrenes and E-1-arylperfluoroalkenes

“…They have also been used as potential enzyme inhibitors [4][5][6] and proved to have cytotoxic activity [7,8]. Some of them have been shown to exhibit potent nematocidal and insecticidal activities [9][10][11][12].…”

An efficient room temperature preparation of bromo difluorovinylzinc reagent (CF2CBrZnCl) and a high yield one-pot synthesis of α-bromo-β,β-difluorostyrenes

“…They can be reduced to 1-monofluoroolefins [1,2]; some of them are potential enzyme inhibitors [3][4][5][6][7] and have exhibited cytotoxic activity [8,9]. Halogen containing 1,1-difluoroalkenes are useful building blocks in organofluorine chemistry not only due to the reactivity of the gem-difluoromethylene unit towards nucleophilic reagents but also due to the possible functionalization at the halogen (chlorine, bromine, iodine) site.…”

CYP17 Inhibitors for Prostate Cancer Treatment – An Update

“…[255]. were also shown to be a potent inhibitors of the enzyme under the same assay conditions ( Table 10, entry 5-7) [258].…”

“…7) with potential for a greater metabolic stability have been reported for CYP17 inhibition [254][255][256][257][258]. Compound 185 was found to inhibit rat testicular CYP17 with an IC 50 of 0.6 M ( Table 9, entry 20) [254].…”