药学学报, 2012, 47(10): 1347-1357
引用本文:
戴厚玲, 郑剑斌, 林 敏, 郑 静, 周福生, 董肖椿, 郭 磊, 刘建文, 闻 韧. 那可丁衍生物合成及其作为微管干扰药物的生物学评估[J]. 药学学报, 2012, 47(10): 1347-1357.
DAI HL,ZHENG JB,LIN Min,ZHENG Jing,ZHOU FS,DONG XC,GUO Lei,LIU JianWen,WEN Ren. Synthesis and biological evaluation of noscapine analogues as microtubule-interfering agents[J]. Acta Pharmaceutica Sinica, 2012, 47(10): 1347-1357.

那可丁衍生物合成及其作为微管干扰药物的生物学评估
戴厚玲1, 郑剑斌1*, 林  敏1, 郑  静1, 周福生2, 董肖椿2, 郭  磊1, 刘建文1, 闻  韧1, 2
(1. 华东理工大学药学院, 上海市新药设计重点实验室, 上海 200237; 2. 复旦大学药学院, 上海 201203)
摘要:

2-羟基-3-甲氧基苯甲醛为原料, 13步反应合成了26个那可丁衍生物。以HL-60细胞为靶细胞, 采用MTT法进行了初步的体外抗肿瘤活性研究。结果表明, 大多数化合物对HL-60细胞株显示出较好的抑制活性和对微管聚合的抑制作用。优选出的化合物31HL-60细胞株以及微管聚合的抑制活性是那可丁的3倍并诱导HL-60细胞在G2/M期累积, 这为那可丁及其衍生物的抗肿瘤活性构效关系的研究打下了基础, 值得进一步研究。

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Synthesis and biological evaluation of noscapine analogues as microtubule-interfering agents
Abstract:

A series of noscapine analogues have been synthesized via 13-step reaction starting from 2-hydroxy-3-methoxybenzaldehyde.  Anti-tumor activities of these compounds were evaluated against HL-60 cell lines in vitro by the standard MTT assay.  It was found that most of these derivatives showed appreciable inhibitory activity against HL-60 and tubulin polymerization.  The results also indicated that the potency of compound 31 is about three times more than that of noscapine against HL-60 cell line and tubulin polymerization.  Moreover, it induced a massive accumulation of cells in G2/M phase.  These results showed noscapine and its derivatives were worth to be intensively studied further.

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