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学科主题: 药学
题名:
New class of potent antitumor acylhydrazone derivatives containing furan
作者: Cui, Zining1; Li, Ying1; Ling, Yun1; Huang, Juan1; Cui, Jingrong2; Wang, Ruiqing2; Yang, Xinling1
关键词: Acylhydrazone ; Synthesis ; Antitumor activity ; Configurational isomer ; Toxicity
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2010-12-01
DOI: 10.1016/j.ejmech.2010.09.007
卷: 45, 期:12, 页:5576-5584
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: IRON CHELATORS ; CELL-LINES ; ADVANCED NEUROBLASTOMA ; REDOX ACTIVITY ; COMPLEXES ; DEFEROXAMINE ; LIGANDS ; ANALOGS ; DESIGN ; CYCLOPHOSPHAMIDE
英文摘要:

A pair of chemical isomeric structures of N-acylhydrazone compounds I and II were designed and synthesized. The reaction was carried out with high diastereoselectivity to obtain one configurational isomer in excellent yields. The exact configuration and conformation of IIa and IIe were confirmed by the X-ray single crystal diffraction. The antitumor bioassay revealed that some compounds exhibited excellent activity against the selected cancer cell lines. In particular, IIf (IC50 =16.4 mu M) was better than doxorubicin (IC50=53.3 mu M) against human promyelocytic leukemic cells (HL-60). Their toxicities were predicted in silico. The results showed that compounds II were safe and eligible to be development candidates. IIf showed great promise as a novel lead compound for further anticancer discovery. (C) 2010 Elsevier Masson SAS. All rights reserved.

语种: 英语
所属项目编号: 2010CB126104 ; 2006AA10A201
项目资助者: National Key Project for Basic Research ; National High Technology Research and Development Program of China ; Scientific Research Foundation of the Graduate School of China Agricultural University
WOS记录号: WOS:000285485000004
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/67711
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.China Agr Univ, Coll Sci, Dept Appl Chem, Minist Agr,Key Lab Pesticide Chem & Applicat, Beijing 100193, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Cui, Zining,Li, Ying,Ling, Yun,et al. New class of potent antitumor acylhydrazone derivatives containing furan[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2010,45(12):5576-5584.
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