Discovery of pyrazolo[1,5-a]pyrimidine-3-carbonitrile derivatives as a new class of histone lysine demethylase 4D (KDM4D) inhibitors
Herein we report the discovery of a series of new small molecule inhibitors of histone lysine demethylase 4D (KDM4D). Molecular docking was first performed to screen for new KDM4D inhibitors from various chemical databases. Two hit compounds were retrieved. Further structural optimization and structure-activity relationship (SAR) analysis were carried out to the more selective one, compound 2, which led to the discovery of several new KDM4D inhibitors. Among them, compound 10r is the most potent one with an IC50 value of 0.41?±?0.03?μM against KDM4D. Overall, compound 10r could be taken as a good lead compound for further studies.
The pyrazole derivative or its salt in a pharmaceutical composition containing them
PROBLEM TO BE SOLVED: To provide a novel compound and a pharmaceutical composition useful for treatment and/or prevention of HIV virus infections.SOLUTION: Provided is a pyrazole derivative represented by the general formula (I) or a salt thereof (in the
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Paragraph 0123
(2017/01/26)
HCV INHIBITING BI-CYCLIC PYRIMIDINES
The present invention relates to the use of bi-cyclic pyrimidines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to processes for pre
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Page/Page column 49
(2010/10/20)
Guanosine Analogues. Synthesis of Nucleosides of Certain 3-Substituted 6-Aminopyrazolopyrimidin-4(5H)-ones as Potential Immunotherapeutic Agents
Several guanosine analogues were synthesized in the pyrazolopyrimidine ring system with various substituents at the 3-position.The new analogues prepared here include the CH3 (2-amino-3-methyl-1-β-D-ribofuranosylpyrazolopyrimidin-4(5H)-one,
Bontems, Roger J.,Anderson, Jack D.,Smee, Donald F.,Jin, Ai,Alaghamandan, Hassan A.,et al.
p. 2174 - 2178
(2007/10/02)
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