title: Synthesis and immunostimulatory activity of 8-substituted amino 9-benzyladenines as potent Toll-like receptor 7 agonists.
abstract: Several 9-benzyl adenine derivatives bearing various substituted amines at the 8-position have been prepared and evaluated for interferon induction in peripheral blood mononuclear cells (PBMC) from healthy human donors. The 8-bromoadenine derivative 5 was used as a versatile intermediate for all substitutions. The most active 8-substituted amino compound was found to be the 8-morpholinoethylamino derivative 19 which had an EC(50) in the submicromolar range.
authors.affiliation: Moores Cancer Center, University of California, San Diego, La Jolla, 92093-0820, USA.
authors.forename: Guangyi
authors.initials: G
authors.lastname: Jin
authors.forename: Christina C N
authors.initials: CC
authors.lastname: Wu
authors.forename: Rommel I
authors.initials: RI
authors.lastname: Tawatao
authors.forename: Michael
authors.initials: M
authors.lastname: Chan
authors.forename: Dennis A
authors.initials: DA
authors.lastname: Carson
authors.forename: Howard B
authors.initials: HB
authors.lastname: Cottam
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000586:Amination; D006801:Humans; D007962:Leukocytes / Q000187:drug effects; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D051199:Toll-Like Receptor 7 / Q000819:agonists* / Q000276:immunology*
chemical_list: D051199:Toll-Like Receptor 7; C055872:9-benzyladenine; D000225:Adenine