- 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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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.
- Ma, Ling,Lu, Liping,Zhu, Miaoli,Wang, Qingming,Li, Ying,Xing, Shu,Fu, Xueqi,Gao, Zengqiang,Dong, Yuhui
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p. 6532 - 6540
(2011/08/03)
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- Selective mono- and bis-oxidation of 2,6-bis(hydroxy methyl) phenols with active manganese dioxide
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Selective mono- and bis-oxidations of 2, 6-bis (hydroxy methyl) phenols with active M(n)O2 were realized, giving 2-hydroxy-3- hydroxymethyl benzaldehydes and 2-hydroxyisophthalaldehydes in good yields. The influence of oxidant activity, reaction solvent and temperature on the selectivity were investigated, and favorable conditions developed.
- Xie,Zhang,Yan,Yuan
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- A novel selective oxidation of 5-substituted 2-hydroxy-3-hydroxymethylbenzaldehydes
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5-Substituted 2-hydroxy-1,3-benzenedicarbaldehydes 3 and 5-substituted 3-formyl-2-hydroxbenzoic acids 4 were prepared by selective oxidation of 5-substituted 2-hydroxy-3-(hydroxymethyl)-benzaldehydes 1 in a one-pot reaction. Compounds 1 were reacted with ethylenediamine and copper acetate to produce the complexes 2 as intermediates, in which formyl and phenolic hydroxy groups were protected in the subsequent oxidation step.
- Hu,Hu
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p. 325 - 326
(2007/10/02)
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