Synthesis of novel dual target inhibitors of PARP and HSP90 and their antitumor activities
作者: Shanshan LinLingYu ZhangXiao ZhangZelei YuXiuwang HuangJianhua XuYang LiuLimin ChenLixian Wu
作者单位: 1Department of Pharmacology, School of Pharmacy, Fujian Medical University (FMU), Fuzhou, PR China
2Institute of Materia Medica, Fujian Medical University (FMU), Fuzhou, PR China
3Fujian Key Laboratory of Natural Medicine Pharmacology, Fujian Medical University (FMU), Fuzhou, PR China
4Department of Public Technology Service Center, Fujian Medical University (FMU), Fuzhou, PR China
5Department of Pharmacochemistry, School of Pharmacy, Fujian Medical University (FMU), Fuzhou, PR China
刊名: Bioorganic & Medicinal Chemistry, 2020, Vol.28 (9)
来源数据库: Elsevier Journal
DOI: 10.1016/j.bmc.2020.115434
关键词: PARPHSP90MultitargetAntitumor
原始语种摘要: Abstract(#br)Poly (ADP-ribose) polymerase (PARP) inhibitors have achieved great success in clinical application, especially for the prolonged survival of cisplatin-sensitive ovarian cancer patients. However, there are still many patients who do not respond to PARP inhibitors. Novel PARP inhibitors with higher activity are urgently needed. Herein we report a series of compounds by molecular hybridization PARP-1 inhibitor Olaparib (Ola) with HSP90 inhibitor C0817 (one curcumin derivative). All synthesized compounds were evaluated for their antiproliferative activity in vitro, and some were further assessed for their inhibitory activities of the PARP enzyme and HSP90 affinity. Our results indicated that compound 4 could bind to HSP90 and cause static quenching, indicating that compound 4 was...
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
  • antitumor 抗癌的
  • novel 长篇小说
  • target 目标
  • their 他们的