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Issue 24, 2011
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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

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Abstract

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 11 and 22 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 11 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.

Graphical abstract: 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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Publication details

The article was received on 31 Jan 2011, accepted on 11 Apr 2011 and first published on 24 May 2011


Article type: Paper
DOI: 10.1039/C1DT10169B
Citation: Dalton Trans., 2011,40, 6532-6540
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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

    L. Ma, L. Lu, M. Zhu, Q. Wang, Y. Li, S. Xing, X. Fu, Z. Gao and Y. Dong, Dalton Trans., 2011, 40, 6532
    DOI: 10.1039/C1DT10169B

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