Tetrapyridylporphine bridged crossed tetra-palladium complexes, and preparation method and antitumor activity thereof

A technology of tetrapyridyl porphyrin bridge and pyridyl porphyrin bridge, which is applied in the field of preparation of tetranuclear platinum complexes

Inactive Publication Date: 2012-04-11
SUN YAT SEN UNIV
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  • Abstract
  • Description
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Problems solved by technology

Although the small molecule stabilizers of G-quadruplex DNA have made great progress, how to obtain ligands/complexes of small molec

Method used

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  • Tetrapyridylporphine bridged crossed tetra-palladium complexes, and preparation method and antitumor activity thereof
  • Tetrapyridylporphine bridged crossed tetra-palladium complexes, and preparation method and antitumor activity thereof
  • Tetrapyridylporphine bridged crossed tetra-palladium complexes, and preparation method and antitumor activity thereof

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Experimental program
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Embodiment 1 4

[0031] Preparation of the cross-shaped tetranuclear platinum complex of embodiment 1 tetrapyridyl porphyrin bridge:

[0032] Dissolve 0.40 millimoles of DPA platinum (II) complex in 15 milliliters of water, add 0.40 millimoles of silver nitrate in a dark place under nitrogen protection, stir at 60°C for 36 hours, and centrifuge to discard the precipitate after the reaction is complete. Keep the clear solution. Dissolve 0.10 mmoles of tetrakis(4-pyridyl)porphyrin in 10 ml of trifluoroethanol, and add it dropwise to the above clear liquid. After the addition is complete, add 10 ml of trifluoroethanol to ensure that no turbidity occurs . The reaction solution was reacted at 60°C in the dark for 2 days under the protection of nitrogen. After the reaction was completed, the reaction solution was concentrated under reduced pressure to 5 ml, and an appropriate amount of absolute ethanol and absolute ether were added to immediately precipitate a purple solid, which was centrifuged t...

Embodiment 2

[0034] Example 2 Antitumor activity experiment of tetrapyridyl porphyrin-bridged cruciform tetranuclear platinum complexes:

[0035] Adopt the compound prepared in embodiment 1 to carry out following test:

[0036] Cell lines and culture conditions: The cell lines used in this experiment are as follows: human colorectal carcinoma cells (HCT-8), human gastric adenocarcinoma cells (BGC-823), human melanoma carcinoma cells (A375), human nasopharyngeal carcinoma cells (KB) and human rectal cancer cells (HT-29). The cells were cultured in DMEM medium containing 10% fetal bovine serum, which contained 100 units of penicillin and 100 micrograms of streptomycin per milliliter, and the cells were seeded in a 10 cm diameter petri dish at 37 degrees, 5% CO 2 The cells were cultured in the environment, and passaged by trypsinization when the cells were confluent.

[0037] Cytotoxicity test: Cytotoxicity was measured by MTT method. The cells were digested with 0.25% trypsin into a singl...

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Abstract

The invention relates to a preparation method of tetra-palladium complexes in a crossed structure which synthesize tetrapyridylporphine bridge by using supramolecular self-assembly. The tetra-palladium complexes are possibly used for treating human cancers. The MTT experiment data indicates that the compounds have high antitumor activity. A single-teeth platinum ligand, of which the chloride ion is substituted by nitrate, and a bridging ligand tetrapyridylporphine are subjected to self-assembly, thereby obtaining new potential anticancer drugs with excellent anticancer activity and tumor targeting property. The complexes have excellent tumor cell targeting property, and induce the G-rich sequence of the cancer gene to form a G-quadruplex structure, thereby inhibiting the activity of the telomere enzyme and further having high antitumor activity. In addition, since the preparation method is simple and easy to implement, has lower cost, and can be complemented in a common chemical laboratory, and does not have environment pollution in the production process. Therefore, the tetrapyridylporphine bridged tetra-palladium complexes in a crossed structure can be used as novel potential antineoplastic drugs.

Description

technical field [0001] The present invention relates to a class of quadrinuclear platinum complexes with excellent antitumor activity synthesized by supramolecular self-assembly and tetrapyridyl porphyrin bridges, and a preparation method thereof, in particular to tetranuclear platinum complexes with a cruciform structure Preparation method and its antitumor activity. Background technique [0002] Since G-quadruplex DNA was found to be a potential anti-tumor target, the design of new anti-cancer drugs targeting G-quadruplex DNA has become one of the important frontiers in the research of cancer targeted therapy drugs in recent years. Although the small molecule stabilizers of G-quadruplex DNA have made great progress, how to obtain ligands / complexes of small molecule G-quadruplex DNA with higher affinity and better selectivity is still a challenge. A great challenge for chemists and biologists. Because metal complexes have many incomparable advantages of small organic mole...

Claims

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Application Information

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IPC IPC(8): C07F15/00C07D487/22A61K31/555A61P35/00
CPCC07D487/22C07F15/00A61K31/555A61P35/00C07F15/0093
Inventor 毛宗万郑小辉丁轶良黄华珍计亮年
Owner SUN YAT SEN UNIV
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