期刊文献+

二茂铁基查耳酮类化合物的合成及其抗乳腺癌活性研究 被引量:4

Synthesis of ferrocenyl chalcone compounds and their anti-breast cancer activities
原文传递
导出
摘要 目的设计并合成了二茂铁基查耳酮类化合物,并对其抗乳腺癌活性进行研究。方法通过Claisen-Schmidt缩合反应合成含有二茂铁基的查耳酮类化合物,并通过MTT法对目标化合物的抗乳腺癌活性进行研究。结果合成了9个含有二茂铁基查耳酮类化合物,其结构均通过^1H-NMR、^13C-NMR进行了表征。生物活性结果表明,目标化合物1-9对MCF-7和MDA-MB-23均具有较强的抑制活性,其中化合物6对MDA-MB-231的抑制活性最强。结论本研究为开发具有抗荷尔蒙非依赖型乳腺癌活性的查耳酮类化合物提供了参考。 Objective To design and synthesize ferrocenyl chalcone compounds, and to study their anti-breast cancer activities. Methods A series of ferrocenyl chalcones were synthesized by Claisen-Schmidt condensation reaction, and the anti-breast cancer activity was assessed by MTT method. Results Nine ferrocenyl chalcone compounds were synthesized and characterized by ^1H-NMR and ^13C-NMR. The preliminary biological results showed that target compounds 1 — 9 displayed significant inhibitory activities on both MCF-7 and MDA-MB-231 cell lines. Specifically, compound 6 showed the best inhibitory activity against MDA-MB-231. Conclusion This study provides reference for development of chalcone compounds with inhibitory activity in hormone-independent breast cancer.
作者 陈善龙 谭娟
出处 《现代药物与临床》 CAS 2015年第8期913-916,共4页 Drugs & Clinic
关键词 二茂铁基查耳酮 合成 抗乳腺癌活性 ferrocenyl chalcone synthesis anti-breast cancer activity
  • 相关文献

参考文献12

  • 1Anders C K, Johnson R, Litton J K, et al. Breast cancer before age 40 years[J].Semin Oncol, 2009, 36(3): 237-249.
  • 2Jordan V C. Tamoxifen: a most unlikely pioneering medicine[J].Nat Rev Drug Dis, 2003, 2(3): 205-213.
  • 3Ariazi E A, Ariazi J L, Cordera F, et al. Estrogen receptors as therapeutic targets in breast cancer[J].Curr Top Med Chem, 2006, 6(3): 181-202.
  • 4van Leeuwen F E, Benraadt J, Coebergh J W, et al. Risk of endometrial cancer after tamoxifen treatment of breast cancer[J].Lancet, 1994, 343(8895): 448-452.
  • 5Brzozowski A M, Pike A C W, Dauter Z, et al. Molecular basis of agonism and antagonism in the oestrogen receptor[J].Nature, 1997, 389(6652): 753-758.
  • 6Hortobagyi G N. Treatment of breast cancer[J].N Engl J Med, 1998, 339(14): 974-984.
  • 7Munster P N, Marchion D, Thomas S, et al. Phase I trial of vorinostat and doxorubicin in solid tumours: histone deacetylase 2 expression as a predictive marker[J].Br J Cancer, 2009, 101(7): 1044-1050.
  • 8Cázares Marinero Jde J, Lapierre M, Cavaillès V, et al. Efficient new constructs against triple negative breast cancer cells: synthesis and preliminary biological study of ferrocifen-SAHA hybrids and related species[J].Dalton Trans, 2013, 42(43): 15489-15501.
  • 9Wang Y, Chan F L, Chen S, et al. The plant polyphenol butein inhibits testosterone-induced proliferation in breast cancer cells expressing aromatase[J].Life Sci, 2005, 77(1): 39-51.
  • 10K?pf-Maier P, K?pf H, Neuse E W. Ferricenium complexes: a new type of water-soluble antitumor agent[J].J Cancer Res Clin Oncol, 1984, 108(3): 336-340.

二级参考文献25

  • 1Katzenellenbogen B S, Katzenellenbogen J A. Defining the "S" in SERMs [J]. Science, 2002, 295(5564): 2380- 2381.
  • 2Pennisi E. Differing roles for estrogen's two receptors [J]. Science, 1997, 277(5331): 1439.
  • 3Schaudig D K, Schwenkhagen A. Selektive ostrogenrezepto-rmodulatoren (SERMs) [J]. Gynakologische Endokn'nologie, 2008, 6(4): 205-212.
  • 4Ariazi E A, Ariazi J L, Cordera F, et al. Estrogen receptorsas therapeutic targets in breast cancer [J]. Curt Top Med Chem, 2006, 6(3): 181-202.
  • 5Silverman S L. New selective estrogen receptor modulators (SERMs) in development [J]. Cur Osteoporos Rep, 2010, 8(3): 151-153.
  • 6Cummings S R, Ensmd K, Delmas P D, et al. Lasofoxifene in postmenopausal women with osteoporosis [J]. N Engl J Med, 2010, 362(8): 686-696.
  • 7Lanyon L, Armstrong V, Ong D, et al. Is estrogen receptor a key to controlling bones' resistance to fracture? [J].JEndocrinol, 2004, 182(2): 183-191.
  • 8Yang N N, Bryant H U, Hardikar S, et al. Estrogen and raloxifene stimulate transforming growth factor-beta 3 gene expression in rat bone: a potential mechanism for estrogen- or raloxifene-mediated bone maintenance [J]. Endocrnology, 1996, 137(5): 2075-2084.
  • 9Swan V J, Hamilton C J, Jamal S A. Lasofoxifene in osteoporosis and its place in therapy [J]. Adv Ther, 2010, 27(12): 917-932.
  • 10Borjesson A E, Farman H H, Engdahl C, et al. The role of activation functions 1 and 2 of estrogen receptor-ct for the effects of estradiol and selective estrogen receptor modulators in male mice [J]. J Bone Miner Res, 2013, 28(5): 1117-1126.

共引文献6

同被引文献14

引证文献4

二级引证文献6

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