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Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity
Longjun Ma1,2, Yan Zhou3, Dehua Yang3
1Department of Applied Chemistry, School of Chemistry and Chemical Engineering, Lanzhou Jiaotong University, 88 Anning West Road, Lanzhou 730070, China.
Abstract:
Hydroxymethylthiohydantoin, hydroxymethylthiohydantoin, and hydantoin, containing a pyridine group, were synthesized to study their androgen receptor antagonistic activities. Among them, compounds 6a/6c/7g/19a/19b exhibited excellent androgen receptor antagonistic activity, which was consistent with or even superior to enzalutamide. In addition, compounds 19a and 19b exhibited better antiproliferative activity than enzalutamide in prostate cancer cells. The results show that compound 19a has great potential as a new AR antagonist.
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