1613412-68-2Relevant academic research and scientific papers
Structure-based design and discovery of potent and selective KDM5 inhibitors
Nie, Zhe,Shi, Lihong,Lai, Chon,O'Connell, Shawn M.,Xu, Jiangchun,Stansfield, Ryan K.,Hosfield, David J.,Veal, James M.,Stafford, Jeffrey A.
, p. 1490 - 1494 (2018/04/10)
Histone lysine demethylases (KDMs) play a key role in epigenetic regulation and KDM5A and KDM5B have been identified as potential anti-cancer drug targets. Using structural information from known KDM4 and KDM5 inhibitors, a potent series of pyrazolylpyridines was designed. Structure-activity relationship (SAR) exploration resulted in the identification of compound 33, an orally available, potent inhibitor of KDM5A/5B with promising selectivity. Potent cellular inhibition as measured by levels of tri-methylated H3K4 was demonstrated with compound 33 in the breast cancer cell line ZR-75-1.
HISTONE DEMETHYLASE INHIBITORS
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Paragraph 00410; 00411; 00656; 00657, (2014/06/24)
Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
