ABSTRACT
A series of 5,5-dimethylthiohydantoin derivatives were synthesized and evaluated for androgen receptor pure antagonistic activities for the treatment of hormone refractory prostate cancer. CH4933468 (32d) with a sulfonamide side chain not only exhibited antagonistic activity with no agonistic activity in the reporter gene assay but also inhibited the growth of bicalutamide-resistant cell lines. This compound also inhibited tumor growth of the LNCaP xenograft in mice dose-dependently.
Subject(s)
Androgen Antagonists , Antineoplastic Agents, Hormonal , Carboxylic Acids , Nitriles/chemical synthesis , Sulfonamides/chemical synthesis , Androgen Antagonists/chemical synthesis , Androgen Antagonists/chemistry , Androgen Antagonists/pharmacology , Animals , Antineoplastic Agents, Hormonal/chemical synthesis , Antineoplastic Agents, Hormonal/chemistry , Antineoplastic Agents, Hormonal/pharmacology , Carboxylic Acids/chemical synthesis , Carboxylic Acids/chemistry , Carboxylic Acids/pharmacology , Cell Line, Tumor , Dose-Response Relationship, Drug , Inhibitory Concentration 50 , Male , Mice , Mice, SCID , Molecular Structure , Nitriles/chemistry , Nitriles/therapeutic use , Prostatic Neoplasms/drug therapy , Sulfonamides/chemistry , Sulfonamides/therapeutic use , Thiohydantoins/chemical synthesis , Thiohydantoins/chemistry , Thiohydantoins/pharmacology , Xenograft Model Antitumor AssaysABSTRACT
Torsion of the accessory spleen is a rare entity that can have variable clinical presentations. We report case involving an 11-year-old boy with severe abdominal pain and a mass that was found to be due to infarction of the accessory spleen, which was twisted on its pedicle. CT revealed a low-attenuating mass with peripheral inflammatory changes in the left upper abdomen. The mass was pathologically confirmed as torsion of the ac-cessory spleen with infarction.