C-5'-三唑基-2'-氧杂-3'-氮杂-4'a-碳核苷：合成与生物评价。
C-5'-Triazolyl-2'-oxa-3'-aza-4'a-carbanucleosides: Synthesis and biological evaluation.
机构信息
Dipartimento Scienze del Farmaco e dei Prodotti per la Salute, University of Messina, Via S.S. Annunziata, 98168 Messina, Italy.
Dipartimento di Scienze del Farmaco, University of Catania, Via A. Doria 6, 95125-Catania, Italy.
出版信息
Beilstein J Org Chem. 2015 Mar 9;11:328-34. doi: 10.3762/bjoc.11.38. eCollection 2015.
A novel series of 2'-oxa-3'-aza-4'a-carbanucleosides, featured with a triazole linker at the 5'-position, has been developed by exploiting a click chemistry reaction of 5'-azido-2'-oxa-3'-aza-4'a-carbanucleosides with substituted alkynes. Biological tests indicate an antitumor activity for the synthesized compounds: most of them inhibit cell proliferation of Vero, BS-C-1, HEp-2, MDCK, and HFF cells with a CC50 in the range of 5.0-40 μM. The synthesized compounds do not show any antiviral activity.
一类新型的 2'-氧代-3'-氮杂-4'a-碳核苷类化合物被开发出来，其特征是在 5'-位带有一个三唑连接基团，该化合物通过 5'-叠氮-2'-氧代-3'-氮杂-4'a-碳核苷与取代的炔烃的点击化学反应得到。生物测试表明，所合成的化合物具有抗肿瘤活性：它们中的大多数化合物对 Vero、BS-C-1、HEp-2、MDCK 和 HFF 细胞的增殖具有抑制作用，CC50 值在 5.0-40 μM 范围内。所合成的化合物没有表现出任何抗病毒活性。
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