药学学报, 2013, 48(6): 874-880
引用本文:
袁 明, 李家明, 何广卫, 钟国琛, 张艳春. 丙戊酸水杨酰芳胺酯类化合物的设计、合成及抗肿瘤活性研究[J]. 药学学报, 2013, 48(6): 874-880.
YUAN Ming, LI Jia-ming, HE Guang-wei, ZHONG Guo-chen, ZHANG Yan-chun. Design, synthesis and antitumor activity of valproic acid salicylanilide esters[J]. Acta Pharmaceutica Sinica, 2013, 48(6): 874-880.

丙戊酸水杨酰芳胺酯类化合物的设计、合成及抗肿瘤活性研究
袁 明1, 李家明1*, 何广卫2, 钟国琛1, 张艳春1
(1. 安徽中医药大学药学院, 安徽省现代中药重点实验室, 安徽 合肥 230031; 2. 合肥医工医药有限公司, 安徽 合肥 230088)
摘要:

依据前药原理, 设计合成了系列具有抗肿瘤活性的水杨酰胺酯类化合物, 并通过MS1H NMR 13C NMR确证了目标化合物的结构K562A549A431 3种细胞株为活性筛选对象, 利用MTT法与SRB进行初步的体外抗肿瘤活性研究。结果表明, 化合物6h6j3种细胞株的抑制活性均强于阳性化合物gefitinib, 与原药对照氯硝柳胺相当, 值得进一步研究。

关键词:   
Design, synthesis and antitumor activity of valproic acid salicylanilide esters
Abstract:

A series of valproic acid salicylanilide esters were designed and synthesized based on the principle of prodrug.  The structures of the target compounds were confirmed by MS, 1H NMR and 13C NMR.  Anti-tumor activities of these compounds against K562, A549, A431cells in vitro were investigated by MTT assay and SRB assay.  The results indicated that the compounds 6h6j were found to have stronger cell growth inhibitory action than gefitinib, and comparable to niclosamide, which are worth to be intensively studied further.

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