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标题:Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening.
时间:2020-03-26 20:20:16
DOI:10.1016/j.bmcl.2016.05.047
PMID:27241691
作者:El-Damasy, Ashraf Kareem;Cho, Nam-Chul;Pae, Ae Nim
关键词:2-Anilinoquinolines;Antiproliferative activity;3-(Morpholino)propoxy;3-(4-Methylpiperazin-1-yl)propoxy;TrkA kinase
出版源: 《Bioorganic & Medicinal Chemistry Letters》 :S0960894X16305327
摘要:A series of new 2-anilinoquinolines possessing 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety at C5 of quinoline has been designed and synthesized as potential anticancer agents. Their antiproliferative activities were evaluated against a panel of 60 cancer cell lines at NCI and compared with gefitinib as a reference compound. Most of the tested compounds displayed potent and broad spectrum antiproliferative activities. Compounds7d,7fand7gshowed strong inhibitory and lethal effects at 10μM concentration. Moreover, they manifested superior potencies and efficacies than gefitinib across the most tested cell lines. Compound7d, with 4-chloro-3-trifluoromethylphenyl group, proved to be the most potent and efficacious derivative in this series, with mean GI50and TGI values of 1.62μM and 3.47μM, respectively. Kinase screening of7dagainst a panel of 47 oncogenic kinases revealed its selective inhibitory effect (96% inhibition) towards TrkA kinase. Furthermore, the most potent compounds showed low cytotoxic effects against HFF-1 normal cell line.
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目录:
  • Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening
    • Acknowledgments
    • Supplementary data
    • References and notes

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