title: D-4'-thioadenosine derivatives as highly potent and selective agonists at the human A3 adenosine receptor.
abstract: 4'-Thionucleoside derivatives as potent and selective A3 adenosaine receptor agonists were synthesized, starting from D-gulono-gamma-lactone via D-thioribosyl acetate as a key intermediate, among which the 2-chloro-N6-methyladenosine-5-methyluronamide showed the most potent and selective binding affinity (Ki = 0.28 +/- 0.09 nM) at the human A3 adenosine receptor.
authors.affiliation: College of Pharmacy, Seoul National University, Seoul [corrected] Korea.
authors.forename: Hyouk Woo
authors.initials: HW
authors.lastname: Lee
authors.forename: Dae Hong
authors.initials: DH
authors.lastname: Shin
authors.forename: Ji Young
authors.initials: JY
authors.lastname: Jeong
authors.forename: Hea Ok
authors.initials: HO
authors.lastname: Kim
authors.forename: Moon Woo
authors.initials: MW
authors.lastname: Chun
authors.forename: N
authors.initials: N
authors.lastname: Melman
authors.forename: Z G
authors.initials: ZG
authors.lastname: Gao
authors.forename: Kenneth A
authors.initials: KA
authors.lastname: Jacobson
authors.forename: Lak Shin
authors.initials: LS
authors.lastname: Jeong
mesh_terms: D000085:Acetates / Q000737:chemistry; D000241:Adenosine / Q000031:analogs & derivatives* / Q000737:chemistry; D058909:Adenosine A3 Receptor Agonists; D000818:Animals; D005663:Furans / Q000737:chemistry; D005942:Gluconates / Q000737:chemistry; D006801:Humans; D007700:Kinetics; D007783:Lactones / Q000737:chemistry; D008024:Ligands; D008956:Models, Chemical; D009705:Nucleosides / Q000737:chemistry; D010100:Oxygen / Q000737:chemistry; D011485:Protein Binding; D051381:Rats; D043684:Receptor, Adenosine A3 / Q000737:chemistry*; D013872:Thionucleosides / Q000737:chemistry*
chemical_list: C506205:2-chloro-N(6)-methyladenosine-5'-methyluronamide; D000085:Acetates; D058909:Adenosine A3 Receptor Agonists; D005663:Furans; D005942:Gluconates; D007783:Lactones; D008024:Ligands; D009705:Nucleosides; D043684:Receptor, Adenosine A3; D013872:Thionucleosides; C050070:4'-thioadenosine; D000241:Adenosine; D010100:Oxygen