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Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity.

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.

SUBMITTER: Ma L

PROVIDER: S-EPMC9505067 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature

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Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity.

Ma Longjun L Zhou Yan Y Yang Dehua D Wang Ming-Wei MW Lu Wei W Jin Jiyu J

Molecules (Basel, Switzerland) 20220910 18

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 ...[more]

PMID: 36144603

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