2. Academic Validation
  3. Synthesis and immunostimulatory activity of substituted TLR7 agonists

Synthesis and immunostimulatory activity of substituted TLR7 agonists

  • Bioorg Med Chem Lett. 2016 Sep 1;26(17):4246-9. doi: 10.1016/j.bmcl.2016.07.049.
Babatope Akinbobuyi 1,  Lei Wang 2,  Katherine C Upchurch 3,  Matthew R Byrd 1,  Charles A Chang 4,  Jeremy M Quintana 1,  Rachel E Petersen 1,  Zacharie J Seifert 1,  José R Boquin 5,  SangKon Oh 3,  Robert R Kane 6
Affiliations

Affiliations

  • 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: [email protected].
PMID: 27476423 DOI: 10.1016/j.bmcl.2016.07.049
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.

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