300627-68-3

Upstream product

• 89677-75-8 2-iodo-4-nitrobenzamide 
• 89459-38-1 4-nitro-2-iodobenzoic acid 
• 861602-59-7 2-iodo-4-nitrobenzoyl chloride 
• 300627-48-9 4-amino-2-iodobenzonitrile 
• 300627-43-4 2-iodo-4-nitrobenzonitrile 
• 619-17-0 4-Nitroanthranilic acid 
• 300627-53-6 2-iodo-4-isothiocyanatobenzonitrile 
• 300627-64-9 4-[4,4-dimethyl-3-(4-hydroxybutyl)-5-imino-2-thioxo-1-imidazoldinyl]-2-iodobenzonitrile 

Relevant academic research and scientific papers

Synthesis and structure-activity investigation of iodinated arylhydantoins and arylthiohydantoins for development as androgen receptor radioligands

A series of side-chain derivatives of the arylhydantoin RU 58841 and the arylthiohydantoin RU 59063, wherein the aromatic trifluoromethyl was replaced with iodine, was synthesized for development as radioiodinated androgen receptor (AR) ligands. Compounds having N-(methyl) and N-(hydroxybutyl) side-chains displayed high AR binding affinity (0.71 nM i i = 20-59 nM) towards the rat AR. Side-chains containing bulky lipophilic groups such as, benzyl and phenylpropyl, were poorly tolerated (Ki > 219 nM). Superior AR binding affinities (0.71 nM i 11 nM) were displayed by arylhydantoins and arylthiohydantoin derivatives containing hydroxybutyl or methyl side-chains. The latter compounds are potential candidates for development as radioiodinated AR ligands.

Design, synthesis, and pharmacological characterization of 4-[4,4-Dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]-2-iodoben zonitrile as a high-affinity nonsteroidal androgen receptor ligand

4-[4,4-Dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]-2-trifluo romethylbenzonitrile (RU 59063) is a prototype of a new class of high-affinity nonsteroidal androgen receptor (AR) ligands. The search for a radioiodinated AR ligand prompted us