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Bioorg Med Chem Lett. 2016 Sep 1;26(17):4246-9. doi: 10.1016/j.bmcl.2016.07.049. Epub 2016 Jul 22.

Synthesis and immunostimulatory activity of substituted TLR7 agonists.

Author information

1
Department of Chemistry and Biochemistry, Baylor University, One Bear Place #97348, Waco, TX 76798, USA.
2
Baylor Institute for Immunology Research, Baylor Research Institute, 3434 Live Oak Street, Dallas, TX 75204, USA.
3
Institute of Biomedical Studies, Baylor University, One Bear Place #97224, Waco, TX 76798, USA; Baylor Institute for Immunology Research, Baylor Research Institute, 3434 Live Oak Street, Dallas, TX 75204, USA.
4
Institute of Biomedical Studies, Baylor University, One Bear Place #97224, Waco, TX 76798, USA.
5
Department of Chemistry, Augustana College, 639 38th Street, Rock Island, IL 61201, USA.
6
Institute of Biomedical Studies, Baylor University, One Bear Place #97224, Waco, TX 76798, USA; Baylor Institute for Immunology Research, Baylor Research Institute, 3434 Live Oak Street, Dallas, TX 75204, USA; Department of Chemistry and Biochemistry, Baylor University, One Bear Place #97348, Waco, TX 76798, USA. Electronic address: bob_kane@baylor.edu.

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

PMID:
27476423
DOI:
10.1016/j.bmcl.2016.07.049
[Indexed for MEDLINE]

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