Synthesis and activity of 8-substituted benzo[c]quinolizin-3-ones as dual inhibitors of human 5α-reductases 1 and 2

Some potent dual inhibitors of 5α-reductases 1 and 2, based on the benzo[c]quinolizin-3-one structure and with IC50 values ranging between 93 and 166 nM for both isozymes, were found. The presence of the F atom on the ester moiety at the position 8 was crucial. This result can help in the design of other potent, dual inhibitors to be developed as drugs in the treatment of 5α-reductase related diseases.