AI Article Synopsis
- A new series of compounds based on RU 58841 and RU 59063 were created by replacing the trifluoromethyl group with iodine to explore their use as radioiodinated androgen receptor (AR) ligands.
- Some derivatives, particularly those with cyanomethyl, methoxyethyl, and propenyl side-chains, showed moderate binding affinity to rat AR, with K(i) values between 20-59nM.
- However, larger lipophilic side-chains led to significantly lower binding, while hydroxybutyl and methyl side-chains resulted in superior affinities, making them promising candidates for further development as AR ligands.
Article Abstract
A series of side-chain derivatives of the arylhydantoin RU 58841 and the arylthiohydantoin RU 59063, wherein the aromatic trifluoromethyl group was replaced with iodine, was synthesized for possible development as radioiodinated androgen receptor (AR) ligands. Derivatives containing the cyanomethyl, methoxyethyl and propenyl side-chains displayed moderately high affinity (K(i)=20-59nM) towards the rat AR. Side-chains containing bulky lipophilic groups such as, benzyl and phenylpropyl, were poorly tolerated (K(i)>219nM). Superior AR binding affinities (0.71nM
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http://dx.doi.org/10.1016/j.bmcl.2004.08.031 DOI Listing Publication Analysis
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