A Copper(Ⅱ)Complex Based on N-(4-hydroxybenzyl)-L-serine:Synthesis,Crystal Structure and Inhibitory Activity on PTP1B and TCPTP  被引量:2

A Copper(Ⅱ) Complex Based on N-(4-hydroxybenzyl)-L-serine:Synthesis,Crystal Structure and Inhibitory Activity on PTP1B and TCPTP

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作  者:李艳红 卢丽萍 朱苗力 袁彩霞 冯思思 高增强 

机构地区:[1]Institute of Molecular Science,Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry,Shanxi University [2]Fenyang College Shanxi Medical University,Fenyang [3]Beijing Synchrotron Radiation Facility,Institute of High Energy Physics,Chinese Academy of Sciences

出  处:《Chinese Journal of Structural Chemistry》2016年第11期1686-1693,共8页结构化学(英文)

基  金:Supported by NNSFC(Nos.21271121,21471092,21571118)

摘  要:A novel copper(II) complex with the reduced Schiff base, [Cu(L)2]·H2O (I, HL = N-(4-hydroxybenzyl)-L-serine), was prepared in aqueous solution and characterized by elemental analysis, FT-IR, electrospray ionization mass spectrometry and single-crystal X-ray diffraction. Complex I crystallizes in the orthorhombic system, space group P212121, with a = 8.9040(18), b = 9.1530(18), c = 24.891(5)A^°, V = 2028.6(7) A^°3, Z = 4, C20H26CuN2O9, Mr = 501.97, Dc = 1.644g·cm^3, μ = 1.135 mm^-1, F(000) = 1044, GOOF = 1.194, the final R = 0.0484 and wR = 0.1420 for 6186 observed reflections (I 〉 2σ(I)). In I, two L^- anions are coordinated to the copper ion in tridentate and bidentate chelating modes, respectively, resulting in the coordinated geometry of copper ion to be a distorted square pyramid. The intermolecular hydrogen bonds between the complexes, complexes and lattice water molecules lead to a 2D supramolecular network. The bioactivity of the complex as a potential PTPs inhibitory agent in vitro was investigated, displaying potent inhibition against PTP1B (IC50, 0.27 μM) and TCPTP (IC50, 0.57 μM) with a moderate selectivity.A novel copper(II) complex with the reduced Schiff base, [Cu(L)2]·H2O (I, HL = N-(4-hydroxybenzyl)-L-serine), was prepared in aqueous solution and characterized by elemental analysis, FT-IR, electrospray ionization mass spectrometry and single-crystal X-ray diffraction. Complex I crystallizes in the orthorhombic system, space group P212121, with a = 8.9040(18), b = 9.1530(18), c = 24.891(5)A^°, V = 2028.6(7) A^°3, Z = 4, C20H26CuN2O9, Mr = 501.97, Dc = 1.644g·cm^3, μ = 1.135 mm^-1, F(000) = 1044, GOOF = 1.194, the final R = 0.0484 and wR = 0.1420 for 6186 observed reflections (I 〉 2σ(I)). In I, two L^- anions are coordinated to the copper ion in tridentate and bidentate chelating modes, respectively, resulting in the coordinated geometry of copper ion to be a distorted square pyramid. The intermolecular hydrogen bonds between the complexes, complexes and lattice water molecules lead to a 2D supramolecular network. The bioactivity of the complex as a potential PTPs inhibitory agent in vitro was investigated, displaying potent inhibition against PTP1B (IC50, 0.27 μM) and TCPTP (IC50, 0.57 μM) with a moderate selectivity.

关 键 词:copper(Ⅱ) complex N-(4-hydroxybenzyl)-L-serine crystal structure inhibitor PTP1B TCPTP 

分 类 号:O641.4[理学—物理化学]

 

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