Molecular Interactions of New Pregnenedione Derivatives

January 2003 in “ Chemical and Pharmaceutical Bulletin ”

Marisa Cabeza, Elena Ramı́rez, Eugenio Flores, Norma Valencia, Mauricio Sánchez, Ivonne Heuze, Marisa Cabeza

progesterone derivatives 5α-reductase androgen receptor dihydrotestosterone IC50 Ki hamster prostate progesterone 5-alpha-reductase DHT

Studysummary This study reports that five new progesterone derivatives demonstrated inhibitory activity against the 5α-reductase enzyme and binding affinity for the androgen receptor in an in vitro hamster model.

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The study evaluated the in vitro inhibitory activity of five new progesterone derivatives on the 5α-reductase enzyme and their antagonistic effects on the androgen receptor. The compounds showed varying IC50 values for 5α-reductase inhibition, with compound 3 being the most potent (19 nM). The Ki values indicated that compound 4 had the highest affinity for the androgen receptor, followed by compound 5, dihydrotestosterone, compound 2, compound 3, and compound 1. Overall, all five synthesized compounds were effective 5α-reductase inhibitors and exhibited affinity for the androgen receptor in the hamster prostate.

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