Alkynyl gold(I) phosphane complexes: Evaluation of structure–activity-relationships for the phosphane ligands, effects on key signaling proteins and preliminary in-vivo studies with a nanoformulated complex
作者: Vincent AndermarkKatrin GökeMalte KokoschkaMohamed A. Abu el MaatyChing Tung LumTaotao ZouRaymond Wai-Yin SunElisabet AguilóLuciano OehningerLaura RodríguezHeike BunjesStefan WölflChi-Ming CheIngo Ott
作者单位: 1Institute of Medicinal and Pharmaceutical Chemistry, Technische Universität Braunschweig, Beethovenstrasse 55, 38106 Braunschweig, Germany
2PVZ — Center of Pharmaceutical Engineering, Franz-Liszt-Straße 35A, 38106 Braunschweig, Germany
3Institute of Pharmaceutical Technology, Technische Universität Braunschweig, Mendelssohnstrasse 1, 38106 Braunschweig, Germany
4Gilead Sciences & IOCB Research Center, Department of Computational Chemistry, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, 16610 Prague 6, Czech Republic
5Department of Physical Chemistry, Palacky University, 77146 Olomouc, Czech Republic
6Department of Biology, Institut für Pharmazie und Molekulare Biotechnologie, Ruperto-Carola University of Heidelberg, Im Neuenheimer Feld 364, 69120 Heidelberg, Germany
7State Key Laboratory of Synthetic Chemistry, Chemical Biology Center, The University of Hong Kong, 8/F, The Hong Kong Jockey Club Building for Interdisciplinary Research, 5, Sassoon Road, Pokfulam, Hong Kong
8Department of Chemistry, The University of Hong Kong, Pokfulam Road, Hong Kong
9Departament de Química Inorgànica, Universitat de Barcelona, Martí i Franquès 1-11, 08028 Barcelona, Spain
刊名: Journal of Inorganic Biochemistry, 2016, Vol.160 , pp.140-148
来源数据库: Elsevier Journal
DOI: 10.1016/j.jinorgbio.2015.12.020
关键词: AlkyneCancerFormulationGoldMicroarrayXenograft
原始语种摘要: Abstract(#br)Gold alkynyl complexes with phosphane ligands of the type (alkynyl)Au(I)(phosphane) represent a group of bioorganometallics, which has only recently been evaluated biologically in more detail. Structure–activity-relationship studies regarding the residues of the phosphane ligand (P(Ph) 3 , P(2-furyl) 3 , P(DAPTA) 3 , P(PTA) 3 , P(Et) 3 , P(Me) 3 ) of complexes with an 4-ethynylanisole alkyne ligand revealed no strong differences concerning cytotoxicity. However, a relevant preference for the heteroatom free alkyl/aryl residues concerning inhibition of the target enzyme thioredoxin reductase was evident. Complex 1 with the triphenylphosphane ligand was selected for further studies, in which clear effects on cell morphology were monitored by time-lapse microscopy. Effects on...
全文获取路径: Elsevier  (合作)
影响因子:3.197 (2012)

  • alkynyl 炔基
  • heteroatom 杂原子
  • complexes 联合企业
  • alkyl 烷基
  • alkyne 炔烃
  • challenging 有希望的
  • activity 活度
  • structure 构造
  • furyl 呋喃基
  • solubility 溶度