期刊文献+
任意字段
题名或关键词
题名
关键词
文摘
作者
第一作者
机构
刊名
分类号
参考文献
作者简介
基金资助
栏目信息

萘酰亚胺多胺衍生物的合成及其抗肿瘤活性 被引量：4

Synthesis and Antitumor Activity of Polyamine Derivatives of Naphthalimide
下载PDF
导出
摘要 设计合成了萘酰亚胺的4种新的多胺衍生物并进行了体外抗肿瘤活性测试。结果表明,这些萘酰亚胺衍生物能够嵌入DNA碱基对中,并且比氨萘非特对肿瘤细胞具有更高的毒性和更好的选择性,其中化合物3b对4种肿瘤细胞的抑制IC50值分别为7.80、5.08、9.78和9.27μmol/L;高内涵活细胞成像系统结果显示,这些化合物可能是通过线粒体通路而导致的细胞凋亡。 A series of polyamine derivatives of naphthalimide （3a -3d） to be used as antitumor agents was synthesized. The biological and spectroscopic evaluations showed that compounds 3a -3d could used as DNA intercalators and had stronger cytotoxic activity and better selectivity than those of amonafide against cancer cells in vitro. The ICs0 for antiproliferative activity of compound 3b on four cancer cells were 7.80, 5.08, 9. 78 and 9. 27 p^mol/L, respectively. High content screening （HCS） results revealed that the as-prepared compounds might produce cytotoxicity through apoptosis via mitoehondrial pathway.
作者 罗稳 李展 翟洋洋 谢松强 王超杰
机构地区 河南大学天然药物与免疫工程重点实验室 河南大学化学生物研究所
出处 《应用化学》 CAS CSCD 北大核心 2013年第3期265-270,共6页 Chinese Journal of Applied Chemistry
基金 国家自然科学基金重大研究计划培育项目(90913001)
关键词 萘酰亚胺 DNA嵌入剂 抗肿瘤 高内涵成像 naphthalimide, DNA intercalator, antitumor, high content screening
分类号 O622.6 [理学—有机化学]
  • 相关文献

参考文献18

  • 1O'Brien P J, Irwin W, Diaz D, et al. High Concordance of Drug-induced Human Hepatotoxicity with in vitro Cytotoxicity Measured in a Novel Cell-based Model Using High Content Screening[J. Arch Toxicol,2006,80(9) :580-604.
  • 2] Brafia M F, Ramos A. Naphathalimides as Anticancer Agents : Synthesis and Biological Activity [ J ]. Curr Med Chem, 2001, 1(3) :237-255.
  • 3Lv M,Xu H. Overview of N aphthalimide Analogs as Anticancer Agents [ J ]. Curr Med Chem,2009,16 (36) :4797-4813.
  • 4Van Quaquebeke E, Mahieu T, Dumont P, et al. 2,2,2-Trichloro-N-( { 2-[ 2-(dimethyl-amino) ethyl ] -1,3-dioxo-2,3- dihydro-lH-benzo [ de ] isoquinolin-5-yl t carbamoyl ) acetamide ( UNBS3157 ), a Novel Nonhematotoxic Naphthalimide Derivative with Potent Antitumor Activity[ J]. J Med Chem,2007,50(17) :4122-4134.
  • 5Tumiatti V,Milelli A, Minarini A, et al. Design, Synthesis, and Biological Evaluation of Substituted Naphthalene Imides and Diimides as Anticancer Agent[ J]. J Med Chem,2009,52(23) :7873-7877.
  • 6Bah'on G A, Bermano G, Gordon A, et al. Synthesis, Cytotoxicity and DNA-Binding of Novel Bisnaphthalimidopropyl Derivatives in Breast Cancer MDA-MB-231 Cells[J]. Eur J Med Chem,2010,45(4) :1430-1437.
  • 7Li X L, Lin Y J, Wang Q Q,et al. The Novel Anti-tumor Agents of 4-Triazol-1,8-naphthalimides:Synthesis, Cytotoxicity, DNA Intercalation and Photocleavage [ J ]. Eur J Med Chem, 2011,46 (4) : 1274-1279.
  • 8Tian Z Y, Xie S Q, Mei Z H, et al. Conjugation of Substituted Naphthalimides to Polyamines as Cytotoxic Agents Targeting the Akt/mTOR Signal Pathway [ J ]. Org Biomol Chem,2009,7 ( 22 ) :4651-4660.
  • 9梅子厚,田智勇,马红霞,谢松强,赵瑾,王超杰.萘酰亚胺-多胺缀合物的合成及体外抗癌活性[J].药学学报,2009,44(7):754-757. 被引量：5
  • 10Xie S Q, Li Q,Zhang Y H,et al. NPC-16, a Novel Naphthalimide-polyamine Conjugate, Induced Apoptosis and Autophagy in Human Hepatoma HepG2 Cells and Bel-7402 Cells [ J ]. Apoptosis, 2011,16 (1) :27-34.

二级参考文献34

  • 1Filosa R, Peduto A, Micco SD, et al. Molecular modeling studies, synthesis and biological activity of a series of novel bisnaphthalimides and their development as new DNA topoisomerase II inhibitors [J]. Bioorg Med Chem, 2009, 17:13-24.
  • 2Qian XH, Li ZG, Yang Q. Highly efficient antitumor agents of heterocycles containing sulfur atom: linear and angular thiazonaphthalimides against human lung cancer cell in vitro [J]. Bioorg Med Chem, 2007, 15: 6846-6851.
  • 3Brana MF, Cacho M, Garcia MA, et al. New analogues of amonafide and elinafide, containing aromatic heterocycles: synthesis, antitumor activity, molecular modeling, and DNA binding properties [J]. J Med Chem, 2004, 47: 1391-1399.
  • 4Wang CJ, Delcros JG. Biggerstaff J, et al. Synthesis and biological evaluation of N^1-(anthracen-9-ylmethyl)triamines as molecular recognition elements for the polyamine transporter [J]. J Med Chem, 2003, 46: 2663-2671.
  • 5Wang JH, Xie SQ, Li Y J, et al. Synthesis and evaluation of unsymmetrical polyamine derivatives as antitumor agents [J]. Bioorg Med Chem, 2008, 16: 7005-7012.
  • 6Xie SQ, Cheng PF, Liu GC, et al. Synthesis and bioevaluation of N-(arylalkyl)-homospermidine conjugates [J]. Bioorg Med Chem Lett, 2007, 17: 4471-4475.
  • 7Tian ZY, Xie SQ, Du YW, et al. Synthesis, cytotoxicity and apoptosis of naphthalimide polyamine conjugates as antitumor agents [J]. Eur J Med Chem, 2009, 44: 393-399.
  • 8Li F, Cui JN, Guo LY, et al. Molecular design, chemical synthesis, and biological evaluation of '4-1' pentacyclic aryl/ heteroaryl-imidazonaphthalimides [J]. Bioorg Med Chem, 2007, 15: 5114-5121.
  • 9Mosmann T. Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assays [J]. J Immunol Methods, 1983, 65: 55-63.
  • 10Kamal A, Reddy BSN, Reddy GSK, et al. Design and synthesis of C-8 linked pyrrolobenzodiazepine-naphthalimide hybrids as anti-tumour agents [J]. Bioorg Med Chem Lett, 2002, 12: 1933-1935.

共引文献17

同被引文献12

引证文献4

二级引证文献3

应用化学
2013年 第3期

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部