Search for New Antineoplastic Agents Based on Structural Modifications of Steroidal 5α-Reductase, 17β-Hydroxysteroid Dehydrogenase, and 17α-Hydroxylase/17,20-Lyase Inhibitors

November 2025 in “ Russian Journal of Oncology ”

Vladimir А. Zolottsev, Olga Yu. Reshmina, A.M. Korolchuk, A. Yu. Misharin

5α-reductase 17β-hydroxysteroid dehydrogenase 17α-hydroxylase/17,20-lyase steroidal inhibitors

TLDR Modifying steroidal inhibitors shows promise for developing new cancer treatments.

This review explores the optimization of steroidal inhibitors targeting 5α-reductase, 17β-hydroxysteroid dehydrogenase, and 17α-hydroxylase/17,20-lyase to develop new antineoplastic agents. It presents the structures of 209 new compounds and evaluates their therapeutic potential through laboratory and preclinical data. The findings suggest that structural modifications of these steroidal inhibitors are promising for creating new cancer treatments. The review is based on 92 publications sourced from six databases, focusing on existing inhibitors and excluding non-steroidal ones.

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Search for New Antineoplastic Agents Based on Structural Modifications of Steroidal 5α-Reductase, 17β-Hydroxysteroid Dehydrogenase, and 17α-Hydroxylase/17,20-Lyase Inhibitors

Research cited in this study

research Design, Synthesis, and Biological Evaluation of Novel Androst-3,5-Diene-3-Carboxylic Acid Derivatives as Inhibitors of 5α-Reductase Type 1 and 2

research Design, Synthesis and Biological Evaluation of Novel 3-Oxo-4-Oxa-5α-Androst-17β-Amide Derivatives as Dual 5α-Reductase Inhibitors and Androgen Receptor Antagonists

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

research Steroidal 5α-Reductase and 17α-Hydroxylase/17,20-Lyase (CYP17) Inhibitors Useful in the Treatment of Prostatic Diseases

research A Review on Steroidal 5α-Reductase Inhibitors for Treatment of Benign Prostatic Hyperplasia

research An Overview on 5α-Reductase Inhibitors

research Novel C-6 Substituted and Unsubstituted Pregnane Derivatives as 5α-Reductase Inhibitors and Their Effect on Hamster Flank Organs Diameter Size

research Steroid 5α-Reductase Inhibitors

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