MEDI 80 |
| Androgen receptor (AR) is a member of the nuclear receptor superfamily and is a key molecular target in the etiology such as the progression of prostate cancer. AR antagonists are useful for the treatment of androgen-dependent prostate cancer. However, the prostate cancer often advances to a hormone-refractory state in which the disease progressed in the presence of continued androgen ablation or antagonist therapy. AR mutation is considered to be one possible reason for hormone-refractory. For example, the known AR antagonists, hydroxyflutamide and bicartamide show agonistic activity in some AR mutants. In order to overcome the resistance, we designed and synthesized 4-substituted pyrrole-2-carboxamide derivatives as the novel non-steroidal/non-anilide type AR antagonists. Some pyrrole-2-carboxamides inhibited the growth of prostate cancer cells with mutated AR. |
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General Poster Session
7:00 PM-9:00 PM, Sunday, 10 September 2006 Moscone Center -- Hall D, Poster
Sci-Mix
Division of Medicinal Chemistry |