新型核苷类似物：吡啶-4-硫代糖苷的首次合成及其细胞毒性评估。
Novel Nucleoside Analogues: First Synthesis of Pyridine-4-Thioglycosides and Their Cytotoxic Evaluation.
作者信息
Elgemeie Galal, Abou-Zeid Mamdouh, Alsaid Shahinaz, Hebishy Ali, Essa Hanaa
机构信息
a Chemistry Department, Faculty of Science, Helwan University , Helwan , Cairo , Egypt.
b Green Chemistry Department, National Research Center , Dokki , Cairo , Egypt.
出版信息
Nucleosides Nucleotides Nucleic Acids. 2015;34(10):659-73. doi: 10.1080/15257770.2015.1071843. Epub 2015 Oct 13.
The reaction of sodium 2,2-dicyanoethene-1,1-bis(thiolate) with 2-cyano-N-arylacetamides afforded sodium pyridine-4-thiolates, coupling of the latters with 2,3,4,6-tetra-O-acetyl-D-gluco- and D-galactopyranosyl bromides, respectively, afforded new pyridine-4-thioglycosides. Ammonolysis of the latter compounds afforded the free thioglycosides. The antitumor activities of the synthesized compounds were tested against human tumor cell lines; lung (A549), colon (HCT116), liver (HEPG2), and prostate (PC3).
2,2-二氰基乙烯-1,1-双（硫醇盐）钠与2-氰基-N-芳基乙酰胺反应生成吡啶-4-硫醇盐钠，后者分别与2,3,4,6-四-O-乙酰基-D-葡萄糖和D-吡喃半乳糖基溴偶联，得到新的吡啶-4-硫代糖苷。后一种化合物的氨解得到游离硫代糖苷。测试了合成化合物对人肿瘤细胞系的抗肿瘤活性；肺癌（A549）、结肠癌（HCT116）、肝癌（HEPG2）和前列腺癌（PC3）。
Zotero 插件