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题名: Novel ruthenium complexes ligated with 4-anilinoquinazoline derivatives: Synthesis, characterisation and preliminary evaluation of biological activity
作者: Ji, Liyun1, 2;  Zheng, Wei1, 2;  Lin, Yu1, 2;  Wang, Xiuli3;  Lu, Shuang1, 2;  Hao, Xiang1, 2;  Luo, Qun1, 2;  Li, Xianchan1, 2;  Yang, Ling3;  Wang, Fuyi1, 2
关键词: Ruthenium complexes ;  EGFR inhibitors ;  Multi-targeting ;  Anticancer agents ;  MCF-7
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2014-04-01
DOI: 10.1016/j.ejmech.2014.02.062
卷: 77, 页:110-120
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Chemistry, Medicinal
研究领域[WOS]: Pharmacology & Pharmacy
英文摘要: The ruthenium DMSO complexes cis-(RuCl2)-Cl-II(DMO)(4) and [(DMSO)(2)H][trans-(RuCl4)-Cl-III(DMSO)(2)] reacted with 4-(3'-chloro-4'-fluoroanilino)-6-(2-(2-aminoethyl)aminoethoxy)-7-methoxyquinazoline (L1), 4-(3'chloro-4'-fluoroanilino)-6-(2-(1H-imidazol-1-yl)ethoxy)-7-methoxy quinazoline (L2), N-(benzo[d]imidazol-4-yl)-6,7-dimethoxyquinazolin-4-amine hydrochloride (L3), 5-(6,7-dimethoxyquinazolin-4-ylamino)quinolin-8-ol hydrochloride (L4), respectively, to afford [(RuCl2)-Cl-II(DMSO)(2)(L1)] (1), [(RuCl3)-Cl-III(DMSO)(L1)] (2), [(RuCl4)-Cl-III(DMSO)(H-L2)] (3), [(RuCl4)-Cl-III(DMSO)(H-L3)] (4), and [(RuCl3)-Cl-III(DMSO)(H-L4)] (5), which were characterised by mass spectrometry, NMR, elementary analysis and single crystal X-ray diffraction (complex 1). Experimental screening (ELISA) showed that complexes 1, 2 and 3 are remarkably inhibitory towards epidermal growth factor receptor (EGFR) with IC50 values at submicromolar or nanomolar level. Docking studies indicated that complexation with ruthenium has little interference with the formation of the two essential H-bonds between the N3 of the quinazoline ring in Ll and 12 and O-H of Thr766 through a water molecule, and the N1 of the quinazoline ring and N-H of Met769 in EGFR. Moreover, complex 2 was shown to be more active against the EGF-stimulated proliferation of human breast cancer cell line MCF-7 than the better EGFR inhibitor 4-(3'-chloro-4'-fluoroanilino)-6,7-dimethoxyquinazoline, being more potential to induce early-stage apoptosis than gefitinib. These imply that apart from inhibiting EGFR, complex 2 may involve in regulating other biological events related to the proliferation of MCF-7, implicating a novel type of multi-targeting metal-based anticancer agents. (C) 2014 Elsevier Masson SAS. All rights reserved.
关键词[WOS]: PROTEIN-KINASE INHIBITORS ;  CANCER-CELL-LINES ;  DNA-BINDING ;  IN-VITRO ;  NAMI-A ;  ARENE COMPLEXES ;  CHEMICAL SPACE ;  ANTICANCER ACTIVITY ;  METAL-COMPLEXES ;  CYTOTOXICITY
语种: 英语
WOS记录号: WOS:000335874800013
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/145437
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Bing Natl Lab Mol Sci, Beijing, Peoples R China
2.Chinese Acad Sci, Inst Chem, CAS Key Lab Analyt Chem Living Biosyst, Beijing 100190, Peoples R China
3.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China

Recommended Citation:
Ji, Liyun,Zheng, Wei,Lin, Yu,et al. Novel ruthenium complexes ligated with 4-anilinoquinazoline derivatives: Synthesis, characterisation and preliminary evaluation of biological activity[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2014,77:110-120.
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