1,3-Disubstituted-1,2,4-triazin-6-ones with potent activity against androgen receptor-dependent prostate cancer cells

[Display omitted] Synthesis and biological evaluation of a small, focused library of 1,3-disubstituted-1,2,4-triazin-6-ones for in vitro inhibitory activity against androgen-receptor-dependent (22Rv1) and androgen-receptor independent (PC3) castration-resistant prostate cancer (CRPC) cells led to hi...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2024-03, Vol.101, p.117634-117634, Article 117634
Main Authors: Zhao, Shiting, Ali, Abdelsalam S., Liu, Xiaomin, Yu, Zhiwei, Kong, Xinyu, Zhang, Yan, Paul Savage, G., Xu, Yong, Lin, Bin, Wu, Donghai, Francis, Craig L.
Format: Article
Language:English
Subjects:
Androgen receptor
Mouse xenograft
Pharmacokinetic
Prostate cancer
SAR
Synthesis
Triazinone
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Summary:[Display omitted] Synthesis and biological evaluation of a small, focused library of 1,3-disubstituted-1,2,4-triazin-6-ones for in vitro inhibitory activity against androgen-receptor-dependent (22Rv1) and androgen-receptor independent (PC3) castration-resistant prostate cancer (CRPC) cells led to highly active compounds with in vitro IC50 values against 22Rv1 cells of 
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2024.117634