Design, synthesis, and biological evaluation of 3-vinyl-quinoxalin-2(1H)-one derivatives as novel antitumor inhibitors of FGFR1
作者: Liu ZYu SChen DShen GWang YHou LLin DZhang JSYe F
刊名: Drug Design, Development and Therapy, 2016, Vol.2016 (Issue 1), pp.1489-1500
来源数据库: Directory of Open Access Journals
关键词: FGFR1SynthesisQuinoxalinAnti-tumor activityKinase inhibitor.
原始语种摘要: Zhiguo Liu,1,* Shufang Yu,1,* Di Chen,1 Guoliang Shen,1 Yu Wang,1 Leping Hou,2 Dan Lin,1 Jinsan Zhang,1 Faqing Ye1 1School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, 2Second Affiliated Hospital of Zhejiang University School of Medicine, Hangzhou, People’s Republic of China *These authors contributed equally to this work Abstract: FGFR1 is well known as a molecular target in anticancer drug design. TKI258 plays an important role in RTK inhibitors. Utilizing TKI258 as a lead compound that contains a quinazolinone nucleus, we synthesized four series of 3-vinyl-quinoxalin-2(1H)-one derivatives, a total of 27 compounds. We further evaluated these compounds for FGFR1 inhibition ability as well as cytotoxicity against four cancer cell lines (H460, B16-F10, Hela229, and...
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影响因子:3.486 (2012)

  • quinoxalin 灭螨猛
  • synthesis 合成
  • derivatives 派生物
  • vinyl 乙烯基
  • compounds 化合物
  • antitumor 抗癌的
  • activity 活度
  • lines 线型
  • biological 生物学的
  • against 反对