期刊文献+

金刚烷类抗癌药物的合成、结构和初步活性研究 被引量:2

Synthesis,structure and preliminary activity of adamantane derivatives as anticancer agents
原文传递
导出
摘要 将脂溶性好的金刚烷骨架引入到苯乙烯酰胺结构中合成了目标化合物(8a-8c),通过NMR,IR和LC-MS对产物进行结构表征,通过MTS方法初步研究了目标化合物对4种癌细胞增殖活性的影响.MTS实验结果表明,所得的化合物中8c可以有效地抑制癌细胞增殖,对肝癌细胞、宫颈癌细胞和乳腺癌细胞都有很低的IC50值.合成的目标化合物有望进一步研发得到结构新颖、不良反应小的抗肿瘤药物. The target compounds(8 a-8 c)were synthesized by the introduction of lipid-soluble adamantane skeleton into styrylamide structure,and characterized by NMR,IR and LC-MS.The effect of target compounds on the proliferation activity of cancer cells lines was preliminarily studied by MTS assay.The results of MTS showed that obtained compound 8 ccould effectively inhibit the proliferation of cancer cells,and had a low IC50 value for liver cancer cells,cervical cancer cells and breast cancer cells.The target compounds synthesized in this study are expected to be further developed to obtain anti-tumor drugs with novel structure and small adverse reactions.
作者 赵银苹 陈力 侯瑞斌 夏艳 ZHAO Yin-ping;CHEN Li;HOU Rui-bin;XIA Yan(School of Chemistry and Life Science,Changehun University of Technology,Changehun 130012,China;Advanced Institute of Materials Science,Changchun University of Technology,Changchun 130012,China)
出处 《分子科学学报》 CAS CSCD 北大核心 2018年第6期445-451,I0001,共8页 Journal of Molecular Science
基金 国家自然科学基金资助项目(21502008)
关键词 金刚烷 脂溶性 细胞增殖 MTS法 adamantane lipid-soluble cell proliferation MTS assay
  • 相关文献

参考文献3

二级参考文献17

  • 1高治,苏晓明,王艳,井新利.金刚烷的应用开发[J].化工新型材料,2004,32(12):34-35. 被引量:9
  • 2刘红,杨本明.金刚烷胺的临床新用途[J].天津药学,1996,8(3):32-33. 被引量:8
  • 3MALUCCIO M, COVEY A. Recent progress in understanding, diagnosing, and treating hepatoceUular carcinoma[J]. Ca Cancer J Clin ,2012,62 ( 6 ) :394 - 399.
  • 4SIMEONOVA L, GEGOVA G, GALABOV AS. Prophylactic and therapeutic combination effects of rimantadine and osehamivir a- gainst influenza virus A (H3N2) infection in mice [ J]. Antiviral Res, 2012,95(2) :172 - 181.
  • 5LIU J, OBANDO D, LIAO V, et al. The many faces of the ada- mantyl group in drug design[ J]. Eur J Med Chem, 2011,46 (6) :1949 - 1963.
  • 6KAUR G, NARAYANAN VL, RISBOOD PA,et al. Synthesis, structure-activity relationship, and p210 (Bcr-abl) protein tyro- sine kinase activity of novel AG957 analogs [ J ]. Bioorg Med Chem, 2005,13 (5) : 1749 - 1761.
  • 7ALTUCCI L, LEIBOWITZ MD, OGILVIE KM, et al. RAR and RXR modulation in cancer and metabolic disease [ J]. Nat Rev Drug Discovery,2007,6(10) :793 - 810.
  • 8DAWSON MI, HARRIS DL, LIU G,et al. Antagonist analogue of 6-3 '-( 1-adamantyl )--4'-hydroxyphenyl-2-naphthaleneearboxylic acid (AHPN) family of apoptosis inducers that effectively blocks AHPN-induced apoptosis but not cell-cycle arrest [ J]. J Med Chem, 2004,47 ( 14 ) : 3518 - 3536.
  • 9SVINGEN PA, TEFFERI A, KOTTKE TJ, et al. Effect of the Bcr/abl kinase inhibitors AG957 and NSC680410 on chronic my- elogenoasleukemia cells in vitro [ J ] . Clin Cancer Res , 2000,6 ( 1 ) :237 -249.
  • 10SOULE BP, HYODO F, MATSUMOTO K,et al. The chemistry and biology of nitroxide compounds [ J ]. Free Radic Biol Med, 2007, 42(11) :1632 - 1650.

共引文献4

同被引文献26

引证文献2

二级引证文献2

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