Abstract
Fifteen new substituted adenines were synthesized as potential TLR7 agonists. These compounds, along with 9 previously reported compounds, were analyzed for TLR7 activity and for the selective stimulation of B cell proliferation. Several functionalized derivatives exhibit significant activity, suggesting their potential for use as vaccine adjuvants.
Keywords:
Adenine derivatives; Immune activation; Toll-like receptor; Vaccines.
Copyright © 2016 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenine / analogs & derivatives*
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Adenine / chemical synthesis
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Adenine / pharmacology
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Adjuvants, Immunologic / chemical synthesis*
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Adjuvants, Immunologic / chemistry
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Adjuvants, Immunologic / pharmacology
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Amides / chemical synthesis
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Amides / chemistry
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Amides / pharmacology
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B-Lymphocytes / cytology
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B-Lymphocytes / drug effects
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B-Lymphocytes / metabolism
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Cell Proliferation / drug effects
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Cells, Cultured
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Crystallography, X-Ray
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Humans
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Lymphocyte Activation / drug effects
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Molecular Conformation
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Toll-Like Receptor 7 / agonists*
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Toll-Like Receptor 7 / metabolism
Substances
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Adjuvants, Immunologic
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Amides
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Toll-Like Receptor 7
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Adenine