Synthesis of 17β-N-Arylcarbamoylandrost-4-en-3-one Derivatives and Their Anti-Proliferative Effect on Human Androgen-Sensitive LNCaP Cell Line

    June 2016 in “ European Journal of Medicinal Chemistry ”
    Francisco Cortés‐Benítez, Marisa Cabeza, María Teresa Ramírez‐Apán, Berenice Alvarez-Manrique, Eugene Bratoeff
    TLDR Compounds 6f and 6g effectively stop prostate cancer cell growth without harming healthy cells.
    In this study, eight novel 17β-N-arylcarbamoylandrost-4-en-3-one derivatives were synthesized and tested for their anti-proliferative effects on human prostate cancer cell lines, specifically the androgen-sensitive LNCaP and androgen-insensitive PC3 cells. Compounds 6f and 6g demonstrated the highest anti-proliferative activity, achieving 100% inhibition in both cell lines, regardless of androgen presence, and showed low cytotoxicity on healthy rat peripheral blood mononuclear cells. These findings suggested that 6f and 6g could be potent androgen-independent anti-proliferative agents, outperforming existing drugs like finasteride, flutamide, and ketoconazole in this context.
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