3998-88-7Relevant articles and documents
Discovery of a new class of JMJD6 inhibitors and structure–activity relationship study
Wang, Tianqi,Zhang, Rong,Liu, Yang,Fang, Zhen,Zhang, Hailin,Fan, Yan,Yang, Shengyong,Xiang, Rong
supporting information, (2021/05/27)
JmjC domain-containing protein 6 (JMJD6) has been thought as a potential target for various diseases particularly cancer. However, few selective JMJD6 inhibitors have been reported. In this investigation, molecular docking and biological activity evaluation were performed to retrieve new JMJD6 inhibitors, which led to the identification of a hit compound, J2. Further structural optimization and structure–activity relationship (SAR) analysis towards J2 were carried out, which gave a new potent JMJD6 inhibitor, 7p. This compound showed an IC50 value of 0.681 μM against JMJD6, but displayed no activity against other tested JmjC domain-containing protein family members, indicating good selectivity (>100 fold). Collectively, this investigation offers a selective JMJD6 inhibitor, which could be taken as a lead compound for subsequent drug discovery targeting JMJD6.
NOVEL PYRIMIDINE-PYRIDINE DERIVATIVES
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Page/Page column 17, (2011/04/14)
The invention relates to novel pyrimidine-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
Modulators of S1P and Methods of Making And Using
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Page/Page column 63-64, (2010/10/19)
The invention is directed to Compounds of Formula I: as well as methods of making and using the compounds.