title: Synthesis and activity of 8-substituted benzo[c]quinolizin-3-ones as dual inhibitors of human 5alpha-reductases 1 and 2.
abstract: 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.
authors.affiliation: Dipartimento di Chimica Organica Ugo Schiff, Polo Scientifico Università di Firenze, Via della Lastruccia 13, I-50019 Sesto Fiorentino, Italy.
authors.forename: Alessandro
authors.initials: A
authors.lastname: Ferrali
authors.forename: Gloria
authors.initials: G
authors.lastname: Menchi
authors.forename: Ernesto G
authors.initials: EG
authors.lastname: Occhiato
authors.forename: Giovanna
authors.initials: G
authors.lastname: Danza
authors.forename: Rosa
authors.initials: R
authors.lastname: Mancina
authors.forename: Mario
authors.initials: M
authors.lastname: Serio
authors.forename: Antonio
authors.initials: A
authors.lastname: Guarna
mesh_terms: 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*
chemical_list: D058891:5-alpha Reductase Inhibitors; D004791:Enzyme Inhibitors; D007527:Isoenzymes; D011807:Quinolizines