Some potent dual inhibitors of 5alpha-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 5alpha-reductase related diseases.
Synthesis and activity of 8-substituted benzo[c]quinolizin-3-ones as dual inhibitors of human 5alpha-reductases 1 and 2 / A. FERRALI; G. MENCHI; E.G. OCCHIATO; G. DANZA; R. MANCINA; M. SERIO; A. GUARNA. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 15:(2005), pp. 145-148. [10.1016/j.bmcl.2004.10.017]
Synthesis and activity of 8-substituted benzo[c]quinolizin-3-ones as dual inhibitors of human 5alpha-reductases 1 and 2
MENCHI, GLORIA;OCCHIATO, ERNESTO GIOVANNI;DANZA, GIOVANNA;SERIO, MARIO;GUARNA, ANTONIO
2005
Abstract
Some potent dual inhibitors of 5alpha-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 5alpha-reductase related diseases.
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