| 引用本文: | 杜芬,黄剑雄,黄睿,周茵,熊远珍.磷酰胺类化合物的合成及抗K562细胞活性研究[J].中国现代应用药学,2019,36(15):1857-1860. |
| DU Fen,HUANG Jianxiong,HUANG Rui,ZHOU Yin,XIONG Yuanzhen.Synthesis and Anti-K562 Cell Activity of Phosphoramide Compounds[J].Chin J Mod Appl Pharm(中国现代应用药学),2019,36(15):1857-1860. |
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| 摘要: |
| 目的 合成并评价磷酰胺类化合物体外对白血病细胞株K562生物活性的抑制作用。方法 以芳氨基为药效基团，羟脯氨酸为载体设计目标物，通过几步亲核取代反应合成一系列新化合物，并表征其结构。MTT法测定它们对人慢性髓性白血病细胞株K562细胞的抑制作用。结果 发现了10个新化合物有一定的生物活性。结论 发现了一类新的具有一定抗肿瘤活性的磷酰胺类先导化合物。 |
| 关键词: 慢性髓性白血病 酰胺类化合物 合成 K562细胞 |
| DOI：10.13748/j.cnki.issn1007-7693.2019.15.001 |
| 分类号:R914.4 |
| 基金项目:国家自然科学基金项目（81260470）；南昌大学研究生创新基金资助项目（CX2018233） |
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| Synthesis and Anti-K562 Cell Activity of Phosphoramide Compounds |
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DU Fen, HUANG Jianxiong, HUANG Rui, ZHOU Yin, XIONG Yuanzhen
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Medical School of Nanchang University, Nanchang 330006, China
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| Abstract: |
| OBJECTIVE To synthesis and evaluate a series of novel phosphoramide compounds, and to evaluate their in vitro inhibitory activity of leukemia in K562 cells. METHODS The target compounds were designed by using aryl amino as active group while hydroxyproline as carrier moiety, they were synthesized by several nucleophilic substitution reaction, whose structures were characterized, the inhibitory effects of which on human chronic myeloid leukemia cell line K562 were determined by MTT assay. RESULTS Ten new compounds exhibited certain biological activity against K562 cells. CONCLUSION A new class of phosphoramide leading compounds with certain anti-tumor activity is found. |
| Key words: chronic myeloid leukemia phosphoramide compounds synthesis K562 cells |
