新型1-硫杂-4-氮杂螺[4.5]癸烷及其衍生的噻唑并嘧啶和1,3,4-噻二唑硫代糖苷的合成与抗癌活性
Synthesis and Anticancer Activity of New 1-Thia-4-azaspiro[4.5]decane, Their Derived Thiazolopyrimidine and 1,3,4-Thiadiazole Thioglycosides.
作者信息
Flefel Eman M, El-Sayed Wael A, Mohamed Ashraf M, El-Sofany Walaa I, Awad Hanem M
机构信息
Department of Chemistry, College of Science, Taibah University, Al-Madinah Al-Monawarah 1343, Saudi Arabia.
Photochemistry Department, National Research Centre, Dokki 12622, Giza, Egypt.
出版信息
Molecules. 2017 Jan 20;22(1):170. doi: 10.3390/molecules22010170.
New 1-thia-azaspiro[4.5]decane derivatives, their derived thiazolopyrimidine and 1,3,4-thiadiazole compounds were synthesized. The thioglycoside derivatives of the synthesized (1,3,4-thiadiazolyl)thiaazaspiro[4.5]decane and thiazolopyrimidinethione compounds were synthesized by glycosylation reactions using acetylated glycosyl bromides. The anticancer activity of synthesized compounds was studied against the cell culture of HepG-2 (human liver hepatocellular carcinoma), PC-3 (human prostate adenocarcinoma) and HCT116 (human colorectal carcinoma) cell lines and a number of compounds showed moderate to high inhibition activities.
合成了新型1-硫杂-氮杂螺[4.5]癸烷衍生物及其衍生的噻唑并嘧啶和1,3,4-噻二唑化合物。通过使用乙酰化糖基溴的糖基化反应合成了所合成的(1,3,4-噻二唑基)硫杂氮杂螺[4.5]癸烷和噻唑并嘧啶硫酮化合物的硫代糖苷衍生物。研究了所合成化合物对HepG-2（人肝癌细胞）、PC-3（人前列腺腺癌）和HCT116（人结肠直肠癌）细胞系细胞培养物的抗癌活性，许多化合物表现出中度至高抑制活性。
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