title: Synthesis and biological activity of novel 5'-arylamino-nucleosides by microwave-assisted one-pot tandem Staudinger/aza-Wittig/reduction.
abstract: Novel pseudonucleosides with benzylamino group on 5'-position (4) were synthesized by using the microwave-assisted one-pot tandem Staudinger/aza-Wittig/reduction reaction in good yields of 55.2-71.7%. The deacetylation of 4 afforded compounds 5. HIV-1 reverse transcriptase (RT) inhibitory and antitumor activities were preliminarily evaluated with 5. The results showed that the new pseudonucleosides (5) could effectively inhibit HIV-1 RT activity, but no antitumor activity.
authors.affiliation: Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding 071002, China.
authors.forename: Hua
authors.initials: H
authors.lastname: Chen
authors.forename: Jianpeng
authors.initials: J
authors.lastname: Zhao
authors.forename: Yanan
authors.initials: Y
authors.lastname: Li
authors.forename: Fengjuan
authors.initials: F
authors.lastname: Shen
authors.forename: Xiaoliu
authors.initials: X
authors.lastname: Li
authors.forename: Qingmei
authors.initials: Q
authors.lastname: Yin
authors.forename: Zhanbin
authors.initials: Z
authors.lastname: Qin
authors.forename: Xinhao
authors.initials: X
authors.lastname: Yan
authors.forename: Yanfei
authors.initials: Y
authors.lastname: Wang
authors.forename: Pingzhu
authors.initials: P
authors.lastname: Zhang
authors.forename: Jinchao
authors.initials: J
authors.lastname: Zhang
mesh_terms: D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D008872:Microwaves; D009705:Nucleosides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D010084:Oxidation-Reduction; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D009705:Nucleosides; D018894:Reverse Transcriptase Inhibitors; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase