2-（3-氨基-3-脱氧-β-D-木糖呋喃糖基）噻唑-4-甲酰胺：一种具有强效抗肿瘤活性的新型噻唑呋林类似物。
2-(3-Amino-3-deoxy-beta-D-xylofuranosyl)thiazole-4-carboxamide: a new tiazofurin analogue with potent antitumour activity.
作者信息
Popsavin Mirjana, Spaić Sasa, Svircev Milos, Kojić Vesna, Bogdanović Gordana, Popsavin Velimir
机构信息
Department of Chemistry, Faculty of Sciences, University of Novi Sad, Trg D. Obradovića 3, 21000 Novi Sad, Serbia.
出版信息
Bioorg Med Chem Lett. 2006 Oct 15;16(20):5317-20. doi: 10.1016/j.bmcl.2006.07.086.
A new tiazofurin analogue, 2-(3-amino-3-deoxy-beta-d-xylofuranosyl)thiazole-4-carboxamide (3), was synthesized starting from d-glucose and evaluated for its in vitro antiproliferative activity against a panel of human tumour cell lines. Compound 3 exhibited the most powerful cytotoxicity against K562 cells, being approximately 100-fold more potent than tiazofurin. This analogue was also active against Jurkat, HT-29 and HeLa malignant cells, with respective IC(50) values being ca. 2-, 27- and 17-fold lower than those observed for tiazofurin. Remarkably, compound 3 did not exhibit any significant cytotoxicity towards normal foetal lung MRC-5 cell line.
一种新的噻唑呋林类似物，2-(3-氨基-3-脱氧-β-D-木糖呋喃糖基)噻唑-4-甲酰胺(3)，以D-葡萄糖为起始原料合成，并对其针对一组人类肿瘤细胞系的体外抗增殖活性进行了评估。化合物3对K562细胞表现出最强的细胞毒性，其效力约为噻唑呋林的100倍。该类似物对Jurkat、HT-29和HeLa恶性细胞也有活性，其IC(50)值分别比噻唑呋林低约2倍、27倍和17倍。值得注意的是，化合物3对正常胎儿肺MRC-5细胞系未表现出任何显著的细胞毒性。
Zotero 插件