PMID: 7539066Jan 1, 1994Paper

Evaluation of some 4-fluoro- and 4-cyano derivatives of delta 4,3-ketosteroids as inhibitors of testosterone 5 alpha-reductase

Journal of Enzyme Inhibition
M JarmanM Hatzis

Abstract

Some 4-fluorinated analogues of 3-oxo-delta 4 steroids and 4-cyano derivatives of progesterone and androstenedione were evaluated as inhibitors of steroid 5 alpha-reductase activity. Inhibitors of this enzyme may be useful in treating prostatic cancer. 4-Fluoroandrostenedione was a modest inhibitor of the rat enzyme (IC50 = 4.08 microM), while 4-cyanoprogesterone was a potent inhibitor of both the rat and human enzymes (IC50 values = 0.045 microM and 0.050 microM respectively). These two steroids were tested in vivo for activity against androgen sensitive organs in WHT mice. 4-Fluoroandrostenedione caused increases in organ weights, suggesting it is an androgen agonist, while the 4-cyano compound displayed modest androgen ablation. Therefore substitutions at the 4-position may produce compounds of therapeutic use in treating prostate cancer.

References

Jan 1, 1992·The Journal of Clinical Investigation·E P JenkinsD W Russell
May 1, 1990·Proceedings of the National Academy of Sciences of the United States of America·S Andersson, D W Russell
Sep 1, 1990·Journal of Medicinal Chemistry·M JarmanM G Rowlands
Dec 1, 1989·Journal of Steroid Biochemistry·S E BarrieM Jarman
Dec 1, 1982·The Journal of Endocrinology·V PetrowA Tantawi

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