Anti-tumor manganese complexes using mitochondria as target point and preparation and use thereof

A technology of manganese complexes and ligands, which is applied in the field of anti-tumor manganese complexes targeting mitochondria and its preparation and application, which can solve the problems of weak recognition function of tumor cells and interference with normal cell DNA functions, etc.

Inactive Publication Date: 2009-03-25
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of these complexes target DNA, and show strong intercalation with calf thymus DNA in vitro, with a bonding constant of 10. 4 -10 5 , most of the complexes have weak recognition function on tumor cells and interfere with the DNA function of normal cells

Method used

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  • Anti-tumor manganese complexes using mitochondria as target point and preparation and use thereof
  • Anti-tumor manganese complexes using mitochondria as target point and preparation and use thereof
  • Anti-tumor manganese complexes using mitochondria as target point and preparation and use thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0036] The ligand (2-dipicolylaminopropionate) (L 1 ) and MnCl 2 Dissolve in ethanol solution at a molar ratio of 1:1, and control at 50°C; the reaction time is 3 hours, and the solution is evaporated to obtain a yellow manganese complex: [L 1 MnCl 2 ]. Yield: 80%. Molecular formula: C 17 h 21 Cl 2 N 3 o 2 Mn. Elemental analysis: found C, 48.40%; H, 4.93%; N, 9.46; Mn, 12.81%; calculated C, 48.03; H, 4.98; N, 9.88; Cl, ​​16.68; Infrared spectrum data (IR, cm-1): 2936, 1735cm -1 , 1624, 1575, 1493, 1035, 841, 806, 506.

[0037] The ligand (2-dipicolylaminopropionic acid) (L 2 ) and MnCl 2 Dissolve in ethanol solution at a molar ratio of 1:1, add 0.25 g of NaOH, control at 48°C; react for 6 hours, distill off methanol to obtain a yellow manganese complex: [L 2 MnCl]. Yield: 78%. 80%. Molecular formula: C 15 h 16 ClN 3 o 2 Mn. Elemental analysis: found C, 55.47%; H, 4.93%; N, 12.86; Mn, 16.61%; calculated C, 55.39%; H, 4.96%; N, 12.92; Infrared spectral data (...

Embodiment 2

[0039] The ligand (2-dipicolylaminopropionate) (L 1 ) and MnCl 2 Dissolve in ethanol solution at a molar ratio of 1:2, and control at 80°C; the reaction time is 2 hours, and the solution is evaporated to obtain a yellow manganese complex: [L 1 MnCl 2 ]. Yield: 50%. Formula C 17 h 21 Cl 2 N 3 o 2 Mn.

[0040] The ligand (2-dipicolylaminopropionic acid) (L 2 ) and MnCl 2 Dissolve in methanol solution at a molar ratio of 1:2, add 0.050 g of NaOH, control at 65°C; react for 10 hours, distill methanol to obtain light yellow manganese complex: [L 2 MnCl 2 ]. Yield: 59%.C 15 h 16 ClN 3 o 2 mn

Embodiment 3

[0042] The ligand (2-dipicolylaminopropionate) (L 1 ) and MnCl 2 Dissolve in aqueous solution at a molar ratio of 1:1, and control at 30°C; the reaction time is 8 hours, and the solution is evaporated to obtain a yellow manganese complex: [L 1 MnCl 2 ]. Yield: 45%. Formula C 17 h 21 Cl 2 N 3 o 2 Mn.

[0043] The ligand (2-dipicolylaminopropionic acid) (L 2 ) and MnCl 2 Dissolve in methanol solution at a molar ratio of 1:1, add 0.40 g of NaOH, and control at 20°C; the reaction time is 3 hours, and the methanol is evaporated to obtain a light yellow manganese complex: [L 2 MnCl]. Yield: 42%. Formula C 15 h 16 ClN 3 o 2 mn

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Abstract

The invention relates to a micromolecule compound having the functions of anti-tumor and autophagy, a preparation method and the application thereof. The micromolecule compound is a manganese complex L<1>MnCl2 and L<2>MnCl, wherein, the L<1> represents 2-double pyridine methyl-amine propionic ether; and the L<2> represents 2-double pyridine methyl-amine monoprop. The micromolecule compound is obtained through chemosynthesis by taking the ligand L<1> or L<2> and the MnCl2 as main materials. The manganese complex of the double pyridine methyl-amine ligand has strong inhibition effects on the growth of tumor cells A549, Hela, HepG-2 and Eca109, can inhibit the swelling of the mitochondrial induced by the calcium ion and induce the apoptosis of the tumor cells by means of autophagy; the micromolecule compound can be taken as new anti-tumor activity medicine which takes the mitochondria as target spot and the tumor cell autophagy agent used for the drug tolerance tumor therapy.

Description

technical field [0001] The invention relates to the technical field of novel small molecule compounds with anti-tumor and autophagy functions and their preparation, in particular to a class of small molecule drugs with new targeted anti-tumor and tumor cell autophagy functions and a preparation method thereof. Background technique [0002] Traditional chemotherapeutic drugs kill tumor cells by destroying the structure of DNA, inhibiting the expression of related proteins, and interfering with the metabolism of tumor tissues. However, the selectivity of chemotherapeutic drugs is poor. While killing tumor cells, it can also cause damage and death of normal cells in the body. Therefore, the research and development of novel, potent, and low-toxic antitumor drugs is an important topic in the field of life sciences. With the application of cisplatin in anti-tumor (Clarke M J, Zhu F, Frasca DR, Chem.Rev., 1999, 99(9): 2511), it has caused an upsurge in the research of inorganic m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F13/00C07D213/36A61K31/555A61P35/00
Inventor 陈秋云黄娟高静郭文洁
Owner JIANGSU UNIV
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