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New class of potent antitumor acylhydrazone derivatives containing furan
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
2010-12-01
DOI10.1016/j.ejmech.2010.09.007
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
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 ; 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
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
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 ; 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
引用统计
被引频次:69[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/67711
专题北京大学药学院
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
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GB/T 7714
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.
APA Cui, Zining.,Li, Ying.,Ling, Yun.,Huang, Juan.,Cui, Jingrong.,...&Yang, Xinling.(2010).New class of potent antitumor acylhydrazone derivatives containing furan.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,45(12),5576-5584.
MLA Cui, Zining,et al."New class of potent antitumor acylhydrazone derivatives containing furan".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 45.12(2010):5576-5584.
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