Synthesis, biological evaluation and molecular modeling study of [1,2,4]-Triazolo[4,3- c ]quinazolines: New class of EGFR-TK inhibitors
新型EGFR-TK抑制剂[1,2,4]-三唑[4,3-c]喹唑啉的合成、生物学评价及分子模拟研究
作者: Wafaa A. EwesMohammad A. ElmorsyShahenda M. El-MesseryMagda N.A. Nasr
作者单位: 1Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, P.O. Box 35516, Mansoura, Egypt
2Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Delta University for Science and Technology, Egypt
刊名: Bioorganic & Medicinal Chemistry, 2020, Vol.28 (7)
来源数据库: Elsevier Journal
DOI: 10.1016/j.bmc.2020.115373
关键词: TriazoloquinazolineSynthesisAntitumor activityEGFR assayApoptosisMolecular docking studies
英文摘要: Abstract(#br)New series of triazolo[4,3- c ]quinazolines were designed, synthesized and their structures were elucidated using different spectroscopic techniques. They were evaluated for their in vitro antitumor activity against HepG2, MCF-7, PC-3, HCT-116 and HeLa cancer cell lines using MTT assay. It was found that all compounds showed variable in vitro cytotoxicity. Distinct derivatives exhibited higher inhibitory activity against the tested cell lines with IC 50 values ranging from 8.27 to 10.68 µM using DOX standard (IC 50 = 4.17–8.87 µM). In vitro epidermal growth factor receptor (EGFR) inhibition assay was performed. Results revealed that compounds 8 , 19 and 21 exhibited worthy EGFR inhibitory activity with IC 50 values ranging from 0.69 to1.8 µM in comparison to the reference...
全文获取路径: Elsevier  (合作)
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影响因子:2.903 (2012)

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关键词翻译
关键词翻译
  • quinazolines 喹唑啉
  • biological 生物学的
  • docking 靠泊
  • modeling 制祝型
  • activity 活度
  • molecular 分子的
  • evaluation 评价
  • study 学习
  • class 
  • assay 试金