Mononuclear copper(ii) complexes with 3,5-substituted-4-salicylidene-amino- 3,5-dimethyl-1,2,4-triazole: Synthesis, structure and potent inhibition of protein tyrosine phosphatases

Ma L.; Lu L.; Zhu M.; Wang Q.; Li Y.; Xing S.; Fu X.; Gao Z.; Dong Y.

首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Mononuclear copper(ii) complexes with 3,5-substituted-4-salicylidene-amino- 3,5-dimethyl-1,2,4-triazole: Synthesis, structure and potent inhibition of protein tyrosine phosphatases

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Mononuclear copper(ii) complexes with 3,5-substituted-4-salicylidene-amino- 3,5-dimethyl-1,2,4-triazole: Synthesis, structure and potent inhibition of protein tyrosine phosphatases

机译：单核铜（ii）与3,5-取代的4-水杨亚基-氨基-3,5-二甲基-1,2,4-三唑的配合物：蛋白质酪氨酸磷酸酶的合成，结构和有效抑制

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Six copper complexes of Schiff base ligands containing 3,5-substituted-4- salicylideneamino-3,5-dimethyl-1,2,4-triazole have been synthesized and well characterized. The structures of complexes 1 and 2 were determined by X-ray crystal analysis. Fluorescence and potentiometric study indicated that in the physiological pH range, one ligand was dissociated from the complexes to form 1:1 mononucleus copper complexes. The complexes potently inhibit protein tyrosine phosphatase 1B (PTP1B), T-cell protein tyrosine phosphatase (TCPTP), megakaryocyte protein tyrosine phosphatase 2 (PTP-MEG2) and Src homology phosphatase 1 (SHP-1) with 3-4 fold selectivity against PTP1B over TCPTP and PTP-MEG2, and 3-9 fold over SHP-1, but display almost no inhibition against Src homology phosphatase 2 (SHP-2). Complex 1 inhibits PTP1B with a competitive model with Ki of 30 nM. Substitution with small groups at the phenyl of the ligand does not obviously influence the inhibitory ability of the complexes.

机译：合成并很好地表征了六个含有3,5-取代的4-水杨基亚氨基-3,5-二甲基-1,2,4-三唑的席夫碱配体的铜配合物。配合物1和2的结构通过X射线晶体分析确定。荧光和电位研究表明，在生理pH范围内，一种配体从配合物中解离形成1：1单核铜配合物。该复合物可有效抑制蛋白酪氨酸磷酸酶1B（PTP1B），T细胞蛋白酪氨酸磷酸酶（TCPTP），巨核细胞蛋白酪氨酸磷酸酶2（PTP-MEG2）和Src同源磷酸酶1（SHP-1），对PTP1B的选择性为3-4倍在TCPTP和PTP-MEG2中，SHP-1比SHP-1高3-9倍，但对Src同源性磷酸酶2（SHP-2）几乎没有抑制作用。复合物1以Ki为30 nM的竞争模型抑制PTP1B。在配体的苯基上被小基团取代不会明显影响复合物的抑制能力。

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《Dalton transactions: An international journal of inorganic chemistry》 |2011年第24期|共9页
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Ma L.; Lu L.; Zhu M.; Wang Q.; Li Y.; Xing S.; Fu X.; Gao Z.; Dong Y.;
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1. Mononuclear copper(ii) complexes with 3,5-substituted-4-salicylidene-amino- 3,5-dimethyl-1,2,4-triazole: Synthesis, structure and potent inhibition of protein tyrosine phosphatases [J] . Ma L., Lu L., Zhu M., Dalton transactions: An international journal of inorganic chemistry . 2011,第24期

机译：单核铜（ii）与3,5-取代的4-水杨亚基-氨基-3,5-二甲基-1,2,4-三唑的配合物：蛋白质酪氨酸磷酸酶的合成，结构和有效抑制
2. Mononuclear complexes of manganese(II),iron(II),cobalt(II),copper(II),and zinc(II),with 4-amino-3,5-bis(pyridin-2-yl)-1,2,4 triazole and tris(2-aminoethyl)amine:crystal structure of[Ni(tren)abpt)](NO_30_2(H_2O)_2.25 [J] . Mohammad Shakir, Shama Parveen, Nishat Begum, Transition Metal Chemistry . 2004,第2期

机译：锰（II），铁（II），钴（II），铜（II）和锌（II）与4-氨基-3,5-双（吡啶-2-基）-1,2的单核配合物，4三唑和三（2-氨基乙基）胺：[Ni（tren）abpt）]（NO_30_2（H_2O）_2.25的晶体结构
3. Probing the dinucleating behaviour of a bis-bidentate ligand: Synthesis and characterisation of some di- and mononuclear cobalt(II), nickel(II), copper(II) and zinc(II) complexes of 3,5-di(2-pyridyl)-4-(1H-pyrrol-1-yl)-4H-1,2,4-triazole [J] . Klingele MH, Boyd PDW, Moubaraki B, European journal of inorganic chemistry . 2006,第3期

机译：探索双齿双配体的成核行为：3,5-二（2-吡啶基）的一些双核和单核钴（II），镍（II），铜（II）和锌（II）配合物的合成和表征）-4-（1H-吡咯-1-基）-4H-1,2,4-三唑
4. Investigation Of Inhibition Efficiency For Bis3-(Trimethoxysilyl) PropylAmine And 1H-1,2,4Triazole-3,5-Diamine With Help DOE [C] . Ozgen Cum, Nur Kicir, Tunc Tueken, European corrosion congress . 2012

机译：辅助DOE研究双3-（三甲氧基甲硅烷基）丙基胺和1H- 1,2,4三唑-3,5-二胺的抑制效率
5. Synthesis, characterization, and reactivity of mononuclear copper nitrogen oxide complexes: Models of the nitrogen oxide interactions in copper proteins and copper-exchanged zeolites [D] . Ruggiero, Christy Ellen. 1995

机译：单核铜氮氧化物配合物的合成，表征和反应性：铜蛋白和铜交换沸石中氮氧化物相互作用的模型
6. 4-Amino-3,5-dimethyl-4H-1,2,4-triazole [O] . Daojin Li, Guo-Chang Wei, Shu-Zhi Song, 2015

机译：4-氨基-3,5-二甲基-4H-1,2,4-三唑
7. Bis[triaqua(1H-1,2,4-triazole-3,5-dicarboxylato-κ2 O 3,N 4)copper(II)] di-μ-aqua-bis[diaqua(1H-1,2,4-triazole-3,5-dicarboxylato-κ2 O 3,N 4)copper(II)] [O] . Xie, Li-Xia, Li, Xin, Xie, Pu-Hui, 2009

机译：Bis [triaqua（1H-1,2,4-三唑-3,5-二羧酸酯-κ2 Ø 3，N 4）铜（II）]di-μ-aqua-bis[diaqua（1H-1,2,4-三唑-3,5-dicarboxylate-κ2 Ø 3，N 4）铜（II）]

Mononuclear copper(ii) complexes with 3,5-substituted-4-salicylidene-amino- 3,5-dimethyl-1,2,4-triazole: Synthesis, structure and potent inhibition of protein tyrosine phosphatases

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