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.View this study on sciencedirect.com →
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.
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.
RU 58841 may treat acne, hair loss, and excessive hair growth.