Journal
MOLECULES
Volume 27, Issue 18, Pages -Publisher
MDPI
DOI: 10.3390/molecules27185867
Keywords
androgen receptor; antagonist; enzalutamide; hydantoin analogs; antiproliferative
Funding
- Personalized Medicines-Molecular Signaturebased Drug Discovery and Development Strategic Priority Research Program of Chinese Academy of Sciences [XDA12020347, XDA12040308]
- Thousand Talents Program in China
- Shanghai Science and Technology Council [16DZ2280100]
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Hydroxymethylthiohydantoin, hydroxymethylthiohydantoin, and hydantoin, all containing a pyridine group, were synthesized to investigate their androgen receptor antagonistic activities. Among them, compounds 6a/6c/7g/19a/19b showed remarkable antagonistic activity against the androgen receptor, comparable to or even surpassing enzalutamide. Additionally, compounds 19a and 19b exhibited superior antiproliferative activity compared to enzalutamide in prostate cancer cells. These findings suggest that compound 19a holds promising potential as a novel AR antagonist.
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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