|本期目录/Table of Contents|

[1]李楠,等.鬼臼毒素脲类衍生物的合成和体外抗癌活性的研究[J].天津医科大学学报,2016,22(03):199.
 LI Nan,ZHAO Yang,WEI Fei,et al.Synthesis and biological evaluation of 4-ureido podophyllotoxin derivatives as anticancer agents [J].Journal of Tianjin Medical University,2016,22(03):199.
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鬼臼毒素脲类衍生物的合成和体外抗癌活性的研究(PDF)
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《天津医科大学学报》[ISSN:1006-8147/CN:12-1259/R]

卷:
22卷
期数:
2016年03期
页码:
199
栏目:
基础医学
出版日期:
2016-05-20

文章信息/Info

Title:
Synthesis and biological evaluation of 4-ureido podophyllotoxin derivatives as anticancer agents
文章编号:
1006-8147(2016)03-0199-05
作者:

?李楠13 赵阳13

?

(1.天津医科大学药学院,天津市临床药物关键技术重点实验室,天津300070; 2.天津中医药大学研究生院,天津300193;3.中国人民武装警察部队后勤学院生药与药剂学教研室,天津300309)
Author(s):
LI Nan13ZHAO Yang13WEI Fei2GAO Chen-guang3CAO Bo3GAO Ying3CHEN Hong13
(1.School of Pharmacy, Tianjin Medical University, Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, Tianjin300070,China;2.Graduate School,Tianjin University of Traditional Chinese Medicine,Tianjin 300193;3.Department of Pharmacognosy, Logistic University of PAP, Tianjin 300309, China)
关键词:
鬼臼毒素NN’-羰基二咪唑抗肿瘤活性
Keywords:
podophyllotoxins urea N N’- carbonyldiimidazole antitumor activity
分类号:
R9
DOI:
-
文献标志码:
A
摘要:
?目的:为了得到抗癌活性更高的抗肿瘤药物,设计、合成新型脲类鬼臼毒素衍生物。方法:以鬼臼毒素或4’-去甲基鬼臼毒素为起始原料经N, N’-羰基二咪唑 (CDI)活化其C-4位氨基,并与仲胺类化合物进行缩合反应,得到鬼臼毒素脲类衍生物,经氢谱和高分辨质谱对其进行结构表征。采用噻唑蓝(MTT)法测试目标化合物对人白血病(K562)和人宫颈癌(Hela)细胞的体外抗肿瘤活性。结果:合成8个新的目标化合物,其中化合物6a增殖抑制活性较强。结论:在鬼臼毒素C-4位引入哌嗪环脲类结构可提高其体外抗肿瘤活性。
Abstract:
Objective: To obtain anticancer agents with higher efficiency through a novel series of 4-ureido podophyllotoxin derivatives. Methods: The novel target compounds were synthesized by reacting podophyllotoxin or 4’-demethylepipodophyllotoxin with secondary amines under catalytic agent N, N’-carbonyldiimidazole(CDI). All the compounds were characterized by 1H-NMR and HR-MS. Meanwhile, MTT assay was used to test their cytotoxicity against K562 and Hela cell lines. Results: Eight novel target compounds were synthesized. Among them, compound 6a exhibits was identified to have stronger inhibition effect. Conclusion: The anticancer activity of podophyllotoxin could be improved when itAs C-4 is combined with the structure of ureido and piperazidine.

参考文献/References:

[1] 杨显志, 邵华, 张玲琪. 鬼臼毒素资源研究现状[J]. 中草药, 2001, (11): 85
[2] Liu X, Zhang L L, Xu X H, et al. Synthesis and anticancer activity of dichloroplatinum (II) complexes of podophyllotoxin[J]. Bioorg Med Chem Lett, 2013, 23(13): 3780
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[7] Zhang Z J, Tian J, Wang L T, et al. Design, synthesis and cytotoxic activity of novel sulfonylurea derivatives of podophyllotoxin[J]. Bioorg Med Chem, 2014, 22(1): 204
[8] Ai T, Shi S Y, Chen L T, et al. Synthesis and anti-tumor activity evaluation of novel podophyllotoxin derivatives[J]. Chinese Chemical Letters, 2013, 24(1): 37.
[9] Cheng W H, Cao B, Shang H, et al. Synthesis and evaluation of novel podophyllotoxin derivatives as potential antitumor agents[J]. ?Eur J Med Chem, 2014, (85): 498
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相似文献/References:

[1]成伟华,牛聪,孙强稳,等.呋喃鬼臼毒素衍生物及其抗肿瘤活性研究[J].天津医科大学学报,2016,22(05):381.
 CHENG Wei-hua,NIU Cong,et al.Synthesis and evaluation of furanoid podophyllotoxin derivatives with? ?anticancer activity[J].Journal of Tianjin Medical University,2016,22(03):381.

备注/Memo

备注/Memo:

基金项目 国家自然科学基金资助项目(30873363);天津市应用基础项目资助(08JCYBJC070000)

作者简介 李楠(1990-),男,硕士在读,研究方向:天然产物结构改造;通信作者:陈虹,E-mail: chenhongtian06@163.com。

更新日期/Last Update: 2016-05-24