吉西他滨衍生物的合成及其体外抗肿瘤活性的研究
Study on the synthesis and in vitro anti-tumor activity of Gemcitabine derivative
作者：李佩纹;郭玲;邓朗;王力;罗诗;杜正午;田伯乐;张志荣;
Author：
收稿日期： 年卷（期）页码：2018,33(02):-122-125
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：吉西他滨;甲酰烷基酯;衍生物;Bx PC-3细胞;胰腺癌;合成;抗肿瘤活性;细胞周期
Key words：
基金项目：国家自然科学基金重大资助项目(批准号:81690261)
中文摘要
目的合成吉西他滨(Gem)的衍生物,并初步研究其体外抗肿瘤活性。方法将Gem与氯甲酸十六烷基酯反应生成吉西他滨甲酰十六烷基酯(Gem-C16),通过细胞增殖、细胞周期及细胞凋亡的实验评价其抗肿瘤活性。结果成功合成了Gem-C16,其对Bx PC-3、AR42J、A549三种肿瘤细胞的增殖均有明显的抑制作用,抗增殖作用显著强于Gem。Gem-C16可引起Bx PC-3细胞S期细胞增加,呈现S期阻滞现象,可明显诱导细胞发生凋亡,对细胞周期的阻滞作用和对细胞凋亡的诱导作用也显著强于Gem。结论衍生物的设计合成路线可行性高,Gem-C16体外抗肿瘤活性较Gem显著提高。
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