Design, synthesis and biological evaluation of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2 H )-one fragment
作者: Hehua XiongJianqing ZhangQian ZhangYongli DuanHan ZhangPengwu ZhengQidong Tang
作者单位: 1Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, PR China
2School of Optoelectronic Science and Engineering, University of Electronic Science and Technology of China (UESTC), Chengdu 610054, PR China
刊名: Bioorganic & Medicinal Chemistry Letters, 2020, Vol.30 (9)
来源数据库: Elsevier Journal
DOI: 10.1016/j.bmcl.2020.127076
关键词: Synthesis4-(Pyridin-4-yloxy)benzamide derivatives5-Methylpyridazin-3(2 H )-oneInhibitorsC-Met
英文摘要: Abstract(#br)A series of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2 H )-one fragment were designed, synthesized, and evaluated for their biological activity. Most compounds showed effective inhibitory activity against cancer cell lines of A549, HeLa and MCF-7. Among them, the most promising compound 40 showed excellent activity against A549, HeLa and MCF-7 cell lines with IC 50 values of 1.03, 1.15 and 2.59 μM, respectively, which was 2.606.95 times more active than that of Golvatinib. The structure-activity relationships (SARs) showed that the introduction of 5-methylpyridazin-3(2 H )-one to “5-atom linker” and the modification of the amide with morpholine group were beneficial for enhancing the inhibitory activity of compounds. In addition, the further...
全文获取路径: Elsevier  (合作)
影响因子:2.338 (2012)

  • benzamide 苯酰胺
  • derivatives 派生物
  • biological 生物学的
  • synthesis 合成
  • evaluation 评价
  • bearing 方位