Synthesis and Activity of 8-Substituted Benzo[c]quinolizin-3-ones as Dual Inhibitors of Human 5α-Reductases 1 and 2

    November 2004 in “ Bioorganic & Medicinal Chemistry Letters ”
    Alessandro Ferrali, Gloria Menchi, Ernesto G. Occhiato, Giovanna Danza, Rosa Mancina, Mario Serio, Antonio Guarna
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    TLDR New compounds were made that effectively block enzymes related to prostate issues and hair loss.
    In a 2005 study, researchers synthesized a series of 8-substituted benzo[c]quinolizin-3-ones to inhibit human 5α-reductase types 1 and 2, enzymes linked to conditions such as benign prostate hyperplasia, androgenic alopecia, and acne. They found that compounds with a fluorine atom at the 8 position on the ester moiety had significant inhibitory effects, with IC50 values between 93 and 166 nM for both enzyme types. The fluorine atom's presence was key to the compounds' activity, indicating potential for the development of new treatments for diseases related to 5α-reductase. The study was biochemical in nature and did not involve human participants.
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