一种电压门控钠通道配体的合成及其体外生物活性评价  

Synthesis and in vitro Biological Evaluation of Novel Voltage-gated Sodium Channel Ligands

作　　者：刘盼和 袁建勇[1] 胡叶敏[1] 王敬[1] 李雁武[1] 

机构地区：[1]重庆医科大学药学院,重庆400016

出　　处：《中国医药工业杂志》2016年第11期1369-1373,共5页Chinese Journal of Pharmaceuticals

摘　　要：在苯妥英钠(A)结构基础上设计了模型B作为新型的钠离子通道配体,合成9个未见文献报道的化合物(1a^1i),并选用人前列腺癌细胞(DU145、PC3)、人乳腺癌细胞(MCF-7、MDB-MB-231和MDB-MB-453)和上皮细胞(926)进行体外生物活性测试。结果显示,化合物1a、1b和1c具有良好的体外抗乳腺癌和前列腺癌活性;1e具有良好的体外抗乳腺癌细胞选择性。A new model B for voltage-gated sodium channel ligands was designed based on the model of phenytoin sodium （A）, and 9 unreported compounds （1a-1i） were synthesized. The results of preliminary bioassay indicated that compounds la, lb and lc had good antiproliferative activity on breast and prostate cancer cell lines, le had both good selectivity and bioactivity for breast cancer cells.

关 键 词：电压门控钠通道 配体 合成 生物活性 抗增殖活性 

分 类 号：R979.19[医药卫生—药品]