Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC).
نویسندگان
چکیده
A structure-activity relationship study was carried out on a series of thiohydantoins and their analogues 14 which led to the discovery of 92 (MDV3100) as the clinical candidate for the treatment of hormone refractory prostate cancer.
منابع مشابه
Adaptive responses of androgen receptor signaling in castration-resistant prostate cancer
Prostate Cancer (PCa) is an important age-related disease being the most common cancer malignancy and the second leading cause of cancer mortality in men in Western countries. Initially, PCa progression is androgen receptor (AR)- and androgen-dependent. Eventually advanced PCa reaches the stage of Castration-Resistant Prostate Cancer (CRPC), but remains dependent on AR, which indicates the impo...
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Androgens and the androgen receptor have been implicated in a number of human diseases and conditions, most notably prostate cancer. [1] Huggins and Hodges in 1941 demonstrated that bilateral orchiectomy or estrogen treatment is an effective treatment for prostate cancer.[2] Based upon their findings, androgen deprivation therapy (ADT) has remained the main therapeutic option for patients with ...
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ورودعنوان ژورنال:
- Journal of medicinal chemistry
دوره 53 7 شماره
صفحات -
تاریخ انتشار 2010