Advance of structural modification of nucleosides scaffold
| Autor: | Jianyi Wang, Yanchun Yin, Lin Xia, Chunxian Liang, Weisen Lan, Chen Dandan, Zou Lianjia |
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| Rok vydání: | 2021 |
| Předmět: |
Drug
Scaffold Coronavirus disease 2019 (COVID-19) media_common.quotation_subject Nucleosides scaffold Phospholipid Antineoplastic Agents Antiviral Agents 01 natural sciences Article Anti-tumor 03 medical and health sciences chemistry.chemical_compound Drug Discovery Prodrugs Antiviral 030304 developmental biology media_common Pharmacology chemistry.chemical_classification 0303 health sciences 010405 organic chemistry Chemistry Organic Chemistry Fatty acid Nucleosides Uracil General Medicine Triazoles Prodrug Combinatorial chemistry 0104 chemical sciences Nucleoside |
| Zdroj: | European Journal of Medicinal Chemistry |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2021.113233 |
| Popis: | With Remdesivir being approved by FDA as a drug for the treatment of Corona Virus Disease 2019 (COVID-19), nucleoside drugs have once again received widespread attention in the medical community. Herein, we summarized modification of traditional nucleoside framework (sugar + base), traizole nucleosides, nucleoside analogues assembled by other drugs, macromolecule-modified nucleosides, and their bioactivity rules. 2′-“Ara”-substituted by –F or –CN group, and 3′-“ara” substituted by acetylenyl group can greatly influence their anti-tumor activities. Dideoxy dehydrogenation of 2′,3′-sites can enhance antiviral efficiencies. Acyclic nucleosides and L-type nucleosides mainly represented antiviral capabilities. 5-F Substituted uracil analogues exihibit anti-tumor effects, and the substrates substituted by –I, –CF3, bromovinyl group usually show antiviral activities. The sugar coupled with 1-N of triazolid usually displays anti-tumor efficiencies, while the sugar coupled with 2-N of triazolid mainly represents antiviral activities. The nucleoside analogues assembled by cholesterol, polyethylene glycol, fatty acid and phospholipid would improve their bioavailabilities and bioactivities, or reduce their toxicities. Graphical abstract This review mainly summarize the effects of structure modification of traditional nucleoside framework (sugar + base), traizole nucleosides, nucleoside analogues assembled by other drugs, macromolecule-modified nucleosides on the antiviral/anti-tumor activity.Image 1 |
| Databáze: | OpenAIRE |
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