Synthesis and activity of 8-substituted benzo[c]quinolizin-3-ones as dual inhibitors of human 5alpha-reductases 1 and 2.
Some potent dual inhibitors of 5alpha-reductases 1 and 2, based on the benzo[c]quinolizin-3-one structure and with IC(50) values ranging between 93 and 166nM 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 5alpha-reductase related diseases.
Ferrali
Alessandro
A
Dipartimento di Chimica Organica Ugo Schiff, Polo Scientifico Università di Firenze, Via della Lastruccia 13, I-50019 Sesto Fiorentino, Italy.
Menchi
Gloria
G
Occhiato
Ernesto G
EG
Danza
Giovanna
G
Mancina
Rosa
R
Serio
Mario
M
Guarna
Antonio
A
D058891:5-alpha Reductase Inhibitors; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007527:Isoenzymes / Q000037:antagonists & inhibitors*; D011807:Quinolizines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D058891:5-alpha Reductase Inhibitors; D004791:Enzyme Inhibitors; D007527:Isoenzymes; D011807:Quinolizines