title: Ligand-mediated highly effective and selective C-N coupling for synthesizing bioactive N-aryltriazole acyclonucleosides.
abstract: N-aryltriazole nucleosides are new chemical entities with potential biological activity. The two phosphor ligands, Synphos and Xantphos, had a selective and effective impact on Pd-catalyzed C-N coupling with the 5- and 3-bromotriazole acyclonucleoside isomers, affording the corresponding and otherwise difficult to achieve N-aryltriazole nucleosides with good to excellent yields. In addition, two of the synthesized nucleosides showed superior anticancer activity against drug-resistant pancreatic cancer, compared to the reference drug gemcitabine.
authors.affiliation: State Key Laboratory of Virology, College of Chemistry and Molecular Sciences, Wuhan University, Wuhan 430072, People's Republic of China.
authors.forename: Yuting
authors.initials: Y
authors.lastname: Fan
authors.forename: Yi
authors.initials: Y
authors.lastname: Xia
authors.forename: Jingjie
authors.initials: J
authors.lastname: Tang
authors.forename: Palma
authors.initials: P
authors.lastname: Rocchi
authors.forename: Fanqi
authors.initials: F
authors.lastname: Qu
authors.forename: Juan
authors.initials: J
authors.lastname: Iovanna
authors.forename: Ling
authors.initials: L
authors.lastname: Peng
mesh_terms: D002244:Carbon / Q000737:chemistry*; D002384:Catalysis; D018360:Crystallography, X-Ray; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D009584:Nitrogen / Q000737:chemistry*; D009705:Nucleosides / Q000138:chemical synthesis*; D014230:Triazoles / Q000737:chemistry*
chemical_list: D008024:Ligands; D009705:Nucleosides; D014230:Triazoles; D002244:Carbon; D009584:Nitrogen