title: Synthesis and immunostimulatory activity of substituted TLR7 agonists.
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.
authors.affiliation: Department of Chemistry and Biochemistry, Baylor University, One Bear Place #97348, Waco, TX 76798, USA.
authors.forename: Babatope
authors.initials: B
authors.lastname: Akinbobuyi
authors.affiliation: Baylor Institute for Immunology Research, Baylor Research Institute, 3434 Live Oak Street, Dallas, TX 75204, USA.
authors.forename: Lei
authors.initials: L
authors.lastname: Wang
authors.affiliation: 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.
authors.forename: Katherine C
authors.initials: KC
authors.lastname: Upchurch
authors.affiliation: Department of Chemistry and Biochemistry, Baylor University, One Bear Place #97348, Waco, TX 76798, USA.
authors.forename: Matthew R
authors.initials: MR
authors.lastname: Byrd
authors.affiliation: Institute of Biomedical Studies, Baylor University, One Bear Place #97224, Waco, TX 76798, USA.
authors.forename: Charles A
authors.initials: CA
authors.lastname: Chang
authors.affiliation: Department of Chemistry and Biochemistry, Baylor University, One Bear Place #97348, Waco, TX 76798, USA.
authors.forename: Jeremy M
authors.initials: JM
authors.lastname: Quintana
authors.affiliation: Department of Chemistry and Biochemistry, Baylor University, One Bear Place #97348, Waco, TX 76798, USA.
authors.forename: Rachel E
authors.initials: RE
authors.lastname: Petersen
authors.affiliation: Department of Chemistry and Biochemistry, Baylor University, One Bear Place #97348, Waco, TX 76798, USA.
authors.forename: Zacharie J
authors.initials: ZJ
authors.lastname: Seifert
authors.affiliation: Department of Chemistry, Augustana College, 639 38th Street, Rock Island, IL 61201, USA.
authors.forename: José R
authors.initials: JR
authors.lastname: Boquin
authors.affiliation: 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.
authors.forename: SangKon
authors.initials: S
authors.lastname: Oh
authors.affiliation: 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.
authors.forename: Robert R
authors.initials: RR
authors.lastname: Kane
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000276:Adjuvants, Immunologic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001402:B-Lymphocytes / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D018360:Crystallography, X-Ray; D006801:Humans; D008213:Lymphocyte Activation / Q000187:drug effects; D008968:Molecular Conformation; D051199:Toll-Like Receptor 7 / Q000819:agonists* / Q000378:metabolism
chemical_list: D000276:Adjuvants, Immunologic; D000577:Amides; D051199:Toll-Like Receptor 7; D000225:Adenine
keywords: Adenine derivatives; Immune activation; Toll-like receptor; Vaccines