[1]覃坚妹,李剑飞,叶鳗仪,等.双醋瑞因氨基膦酸酯类衍生物的合成及抗肿瘤活性研究[J].江西师范大学学报(自然科学版),2013,(05):510-514.
 QIN Jian-mei,LI Jian-fei,YE Man-yi,et al.The Synthesis and Antitumor Activity Evaluation of Diacerein Amino Phosphonate Derivatives[J].,2013,(05):510-514.
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双醋瑞因氨基膦酸酯类衍生物的合成及抗肿瘤活性研究()
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《江西师范大学学报》(自然科学版)[ISSN:1006-6977/CN:61-1281/TN]

卷:
期数:
2013年05期
页码:
510-514
栏目:
出版日期:
2013-10-31

文章信息/Info

Title:
The Synthesis and Antitumor Activity Evaluation of Diacerein Amino Phosphonate Derivatives
作者:
覃坚妹;李剑飞;叶鳗仪;姚贵阳;黄日镇;王恒山
广西师范大学化学与药学学院,药用资源化学与药物分子工程教育部重点实验室,广西桂林541004
Author(s):
QIN Jian-mei;LI Jian-fei;YE Man-yi;YAO Gui-yang;HUANG Ri-zhen;WANG Heng-shan
关键词:
双醋瑞因α-氨基膦酸酯合成抗肿瘤
Keywords:
diacereinα-amino phosphonatessynthesisantitumor
分类号:
O626
文献标志码:
A
摘要:
以大黄酸、氨基膦酸酯为原料,合成4个新型乙酰化大黄酸的α-氨基膦酸酯类衍生物,并利用IR、1H NMR、13C NMR、31P NMR、ESI-MS和元素分析对化合物的结构进行表征.用MTT方法评价它们在体外对人肝癌(HepG-2)、人鼻咽癌(CNE)、人肺腺癌细胞(Spca-2)和人肺腺癌细胞(Hct-116)株的生长抑制活性.新合成的化合物均具有潜在的体外抑制癌细胞生长活性,尤其是化合物4d表现出了最强的抑制活性,且对人正常的脐静脉内皮细胞具有低毒性.
Abstract:
The diacerein amino phosphonate derivatives were synthesized starting from rhein and amino phosphonate to obtain four target compounds.The structures of compopnds were confirmed by IR、H NMR、C NMR 、P NMR、ESI-MS spectra and elementary analyses,and their invitro anticancer activity against the four cancer celllines of HepG-2、CNE、Spca-2、Hct-116 was evlauate by MTT,four compounds were synthesized with the potential inhibitory growth of cancer cells in vitro,especially the compound of 4d showed the significant inhibitory activity,and for HUVEC cell with low toxicity.

参考文献/References:

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备注/Memo

备注/Memo:
973前期计划基金项目(2011CB512005,2012CB723501);国家自然科学基金(81260472,21101035);八桂学者及教育部创新团队基金(IRT1225)
更新日期/Last Update: 1900-01-01