TLDR Scientists created iodinated arylhydantoins and arylthiohydantoins that could potentially be used for imaging prostate cancer. Some versions with specific side-chains showed high potential for this use.
In 2004, researchers Marcian E. Van Dort and Yong-Woon Jung synthesized and investigated iodinated arylhydantoins and arylthiohydantoins as potential androgen receptor radioligands for external diagnostic imaging of prostate cancer tumor sites. They created a series of side-chain derivatives of the arylhydantoin RU 58841 and the arylthiohydantoin RU 59063, replacing the aromatic trifluoromethyl group with iodine. Derivatives with cyanomethyl, methoxyethyl, and propenyl side-chains showed moderately high affinity towards the rat androgen receptor, while those with bulky lipophilic groups like benzyl and phenylpropyl were poorly tolerated. Superior binding affinities were found in derivatives with hydroxybutyl or methyl side-chains, suggesting their potential for development as radioiodinated androgen receptor ligands.
18 citations,
April 2001 in “Bioorganic & Medicinal Chemistry Letters” The nature of the side chain in RU 58841 derivatives greatly affects its AR affinity, with the N-(iodopropenyl) derivative 13 showing the highest AR binding affinity, suggesting its potential for developing high-affinity radioiodinated AR radioligands.
16 citations,
October 1994 in “The Journal of Steroid Biochemistry and Molecular Biology” Two non-steroidal antiandrogens, RU 58841 and RU 56187, form a common metabolite at different rates, which may influence their effects; RU 56187 could be used for prostate cancer treatment and RU 58841 for acne treatment.
49 citations,
January 1994 in “The Journal of Steroid Biochemistry and Molecular Biology” RU 58841 may treat acne, hair loss, and excessive hair growth.
18 citations,
April 2001 in “Bioorganic & Medicinal Chemistry Letters” The nature of the side chain in RU 58841 derivatives greatly affects its AR affinity, with the N-(iodopropenyl) derivative 13 showing the highest AR binding affinity, suggesting its potential for developing high-affinity radioiodinated AR radioligands.
6 citations,
August 2009 in “Mini-reviews in Medicinal Chemistry” Different drugs can treat high male hormone levels in women, but they have various effects and some may harm a fetus.
1 citations,
May 2001 in “Journal of Labelled Compounds and Radiopharmaceuticals” Scientists at the University of Michigan Medical School successfully created a special compound that can be used to improve imaging of prostate cancer.
30 citations,
June 1988 in “Journal of Steroid Biochemistry” Flutamide combined with an LHRH agonist effectively inhibits prostate growth, suggesting it could treat prostate cancer.
8 citations,
January 1987 in “Gynecological Endocrinology” Flutamide, an antiandrogen, has minimal impact on female rat endocrine systems and does not significantly change their reproductive cycles.
