Synthesis and biological activity of novel 5′-arylamino-nucleosides by microwave-assisted one-pot tandem Staudinger/aza-Wittig/reduction
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- 作者：Hua Chen ; Jianpeng Zhao ; Yanan Li ; Fengjuan Shen ; Xiaoliu Li ; Qingmei Yin ; Zhanbin Qin ; Xinhao Yan ; Yanfei Wang ; Pingzhu Zhang ; Jinchao Zhang
- 关键词：Pseudonucleosides ; Staudinger/aza-Wittig/reduction ; Microwave-assisted ; HIV-RT inhibitory ; Antitumor
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2011
- 出版时间：1 January 2011
- 年：2011
- 卷：21
- 期：1
- 页码：574-576
- 全文大小：202 K
文摘
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.