Abstract
A series of pyrimidine based inhibitors of PDE7 are discussed. The synthesis, structure-activity relationships (SAR) and selectivity against several other PDE family members as well as activity in T cells are presented. These compounds were found to have effects on T cell proliferation, however it is not clear whether the mechanism is related to PDE7 inhibition.
MeSH terms
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Animals
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Cell Proliferation / drug effects
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Cyclic Nucleotide Phosphodiesterases, Type 7 / antagonists & inhibitors*
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Cyclic Nucleotide Phosphodiesterases, Type 7 / genetics
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Cyclic Nucleotide Phosphodiesterases, Type 7 / metabolism
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Gene Knockout Techniques
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Mice
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Phosphodiesterase Inhibitors / chemical synthesis
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Phosphodiesterase Inhibitors / chemistry*
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Phosphodiesterase Inhibitors / pharmacology
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry*
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Pyrimidines / pharmacology
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Structure-Activity Relationship
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T-Lymphocytes / drug effects*
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T-Lymphocytes / immunology
Substances
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Phosphodiesterase Inhibitors
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Pyrimidines
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Cyclic Nucleotide Phosphodiesterases, Type 7