|本期目录/Table of Contents|

[1]蔡文玺,王润玲,董卫莉.新型含吡啶基吡唑酰胺类化合物的合成与抗肿瘤活性[J].天津医科大学学报,2016,22(02):115-118.
　CAI Wen-xi,WANG Run-ling,DONG Wei-li,et al.Synthesis and biological activity of novel amides containing 1-(pyridin-2-yl) pyrazole derivatives[J].Journal of Tianjin Medical University,2016,22(02):115-118.
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新型含吡啶基吡唑酰胺类化合物的合成与抗肿瘤活性(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02期
页码:
115-118
栏目:
基础医学
出版日期:
2016-03-20

文章信息/Info

Title:
Synthesis and biological activity of novel amides containing 1-(pyridin-2-yl) pyrazole derivatives
文章编号:
1006-8147（2016）02-0115-04
作者:

蔡文玺1; 王润玲1; 董卫莉1
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(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. 中国医学科学院药物研究所,国家药物筛选中心,北京 100050)
Author(s):
CAI Wen-xi1;  WANG Run-ling1;  DONG Wei-li1;  LIU Ai-lin2
(1. School of Pharmacy, Tianjin Medical University, Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, Tianjin 300070, China; 2. Institute of Materia Medica, Chinese Academy of Medical Sciences, National Center for Pharmceuticalscreening, Beijing 100050, China)
关键词:
吡唑酰胺类; 合成; 抗肿瘤活性
Keywords:
amides containing 1-(pyridin-2-yl) pyrazole; synthesis; anticancer activity
分类号:
R9
DOI:
-
文献标志码:
A
摘要:

目的 :设计合成一系列新型的含吡啶基吡唑酰胺类化合物，并测试其生物活性。方法:以取代氨基苯甲酸和吡唑羧酸为起始原料，设计并合成了含吡啶基吡唑酰胺类化合物，测试化合物4a~4d对人肺癌A-549，人肝癌Bel7402和人肠癌HCT-8细胞的体外抗肿瘤活性。结果:合成了4个结构全新的含吡啶基吡唑酰胺类化合物，其结构通过 1H NMR、红外光谱和元素分析进行了表征。体外抗肿瘤活性实验研究表明，化合物4d对Bel7402细胞株在浓度为5 ?g/mL时有较好的抑制活性，其他化合物也表现出一定的抑制活性。结论:化合物4d显示了较好的抑癌作用，值得进一步研究。

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Abstract:
Objective: To design and synthesize a series of novel amides containing 1-(pyridin-2-yl) pyrazole derivatives, and to evaluate their biological activities in vitro. Methods: A series of amides containing 1-(pyridin-2-yl) pyrazole derivatives were synthesized using substituted aminobenzoic acid and pyrazole carboxylic acid as starting materials and the biological activity of the title compounds 4a~4d were tested against A-549, Bel7402 and HCT-8 cell lines. Results: Four new types of amides containing 1-(pyridin-2-yl) pyrazole derivatives were synthesized and characterized by 1H NMR, IR and Elemental Analysis．The preliminary results indicated that the compound 4d showed inhibiting effects on Bel7402 cell line in vitro at the concentration of 5 ?g/mL, while showing no notable inhibiting activity against other cell 1ines．Conclusion: Compound 4d may have anticancer activity, and is worth further studying.

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参考文献/References:

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[11] 孙强稳，王杰，方唯硕,等. 新型酰胺类鬼臼毒素衍生物的合成及体外抗肿瘤活性[J]. 天津医科大学学报，2015, 21(4): 282

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备注/Memo

备注/Memo:
基金项目 国家自然科学基金青年基金资助项目(21102103)，中国博士后科学基金特别资助项目(2014T70222 )
作者简介 蔡文玺(1989-)，男，硕士在读，研究方向：药物化学；
通信作者：董卫莉，E-mail: dongweili@tijmu.edu.cn；刘艾林，E-mail:liuailin@imm.ac.cn。
更新日期/Last Update: 2016-03-23