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新型CDDO衍生物的合成及抗肿瘤活性研究
投稿时间:2017-03-31  修订日期:2017-04-12  点此下载全文
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作者单位E-mail
裴江鸿 中国药科大学 1090524551@qq.com 
肖余 中国药科大学  
李其星 中国药科大学  
赵子豪 中国药科大学  
陈莉 中国药科大学 chenli627@cpu.edu.cn 
中文摘要:对2-氰基-3,12-二氧代齐墩果烷-1,9(11)-二烯-28-羧酸(CDDO)进行结构修饰,通过不同连接臂将多种含氮杂环引入C-17位羧基,设计并合成了12个未见文献报道的新化合物(9a~9l),其结构经ESI-MS和1H-NMR确认。采用MTT法评价了化合物对HCT-116、A549及HepG2肿瘤细胞的抑制活性。实验结果表明,部分化合物对肿瘤细胞具有较高的抑制活性,其中化合物9c的活性最强,高于阳性对照药CDDO-Im。血浆稳定性实验表明,化合物9c的血浆稳定性较高,显著高于CDDO-Im。
中文关键词:2-氰基-3,12-二氧代齐墩果烷-1,9(11)-二烯-28-羧酸  衍生物  合成  抗增殖活性  血浆稳定性
 
Synthesis and Antitumor Activity of Novel CDDO Derivatives
Abstract:Twelve novel 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO) derivatives were designed and synthesized (9a~9l) by introducing different heterocyclic rings to 17-COOH of CDDO through various linkers. Their structures were determined by ESI-MS and 1H NMR. The antiproliferative activity of the synthetic derivatives against human cancer cells HCT-116, A549 and HepG2 was evaluated by MTT assay. The experimental results showed that compound 9c was the most potent one,whose antiproliferative activity was stronger than that of the positive control CDDO-Im. Moreover, rat plasma stability assay showed that compound 9c was more stable than CDDO-Im.
keywords:CDDO  derivative  synthesis  antiproliferative activity  plasma stability
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