State Key Laboratory of Virology, College of Chemistry and Molecular Sciences, Wuhan University, Wuhan 430072, People's Republic of China.
Org Lett. 2010 Dec 17;12(24):5712-5. doi: 10.1021/ol102537p. Epub 2010 Nov 18.
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.
N-芳基三唑核苷是具有潜在生物活性的新化学实体。两种膦配体，Synphos 和 Xantphos，对 Pd 催化的 C-N 偶联具有选择性和有效性，与 5-和 3-溴代三唑环核苷异构体反应，得到相应的、否则难以获得的 N-芳基三唑核苷，产率良好至优秀。此外，合成的两种核苷在抗药性胰腺癌方面显示出优于参考药物吉西他滨的抗癌活性。
