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Organic hydridized tetra-core platinum complex and preparation method thereof as well as application technology field of complex in antitumor medicament preparation

A technology of organic hybridization and platinum complexes, applied in platinum group organic compounds, platinum organic compounds, antitumor drugs, etc., to achieve excellent antitumor activity

Inactive Publication Date: 2011-11-23
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far most of the small molecules that stabilize G-quadruplex DNA are organic compounds, and only a small part are metal complexes

Method used

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  • Organic hydridized tetra-core platinum complex and preparation method thereof as well as application technology field of complex in antitumor medicament preparation
  • Organic hydridized tetra-core platinum complex and preparation method thereof as well as application technology field of complex in antitumor medicament preparation
  • Organic hydridized tetra-core platinum complex and preparation method thereof as well as application technology field of complex in antitumor medicament preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Synthesis of organic hybrid tetranuclear platinum complex with cisplatin as auxiliary ligand and bridging ligand of formula (III):

[0030] Formula (III)

[0031] Dissolve 0.3 millimoles of cisplatin in 6 milliliters of water, add 0.6 millimoles of silver nitrate in a dark place under the protection of nitrogen, and stir at 40°C for 15 hours. After the reaction is completed, centrifuge to discard the precipitate and keep the clear night; 0.3 mmol of bridging ligand (L 1 ), the entire reaction was reacted for 5 days at 60°C under the protection of nitrogen and protected from light. After the reaction, a large amount of absolute ethanol was added to the reaction solution to precipitate a pale yellow solid, which was centrifuged to obtain a pale yellow solid, and the product was dried in vacuum. Yield: 63%. Elemental analysis(%),

[0032] Theoretical value: C 32 H 48 N 24 O 24 Pt 4 ·5H 2 O (2021.24): C, 19.00; H, 2.89; N, 16.61. Experimental value: C, 19.36; H, 3.08; N, 16.53....

Embodiment 2

[0036] The anti-tumor activity test and results of the compound prepared in Example 1.

[0037] Cell lines and culture conditions: HepG2 (human liver cancer cell line), Hela (human cervical cancer cell line), MCF-7 (human breast cancer cell line), A549 (human lung cancer cell), A549 / cisR (cisplatin-resistant lung cancer cell) ) Provided by the Laboratory and Animal Center of Sun Yat-sen University. 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. After the cells were inoculated in a petri dish with a diameter of 10 cm, 37 degrees, 5% CO 2 Cultivation in the environment, when the cells are full, trypsinization is used for passage.

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Abstract

The invention relates to an organic hydridized tetra-core platinum complex having an anticancer activity. The structure general formula of the complex is shown in a formula (I), wherein in the formula (I), a bond (as shown in the specification) represents the same bridge ligand which is one of formulas (II), (III) and (IV). The compound has excellent antitumor activity, and especially, a methyl thiazolyl tetrazolium (MTT) test data of human lung cancer cell A549 / cisR shows that the antitumor activity of the compound is 10 times that of cisplatinum.

Description

[0001] The present invention relates to a class of tetranuclear platinum complexes that use supramolecular self-assembly to synthesize organic hybrids and have excellent anti-tumor activity and a preparation method thereof, in particular to a preparation method of tetranuclear platinum complexes with amino side arms and their anti-tumor activity. tumor activity. Background technique [0002] Since the discovery of G-quadruplex DNA as a potential antitumor target, a great deal of work has been done on small organic molecules that can stabilize G-quadruplex DNA. But so far most of the small molecules that stabilize G-quadruplex DNA are organic compounds, and only a small part are metal complexes. Because metal complexes have many incomparable advantages of small organic molecules, such as rigid and flexible geometric structure changes and rich electrochemical properties, they also have optical, magnetic and catalytic properties. In terms of binding mode, metal complexes can no...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/555A61P35/00
CPCA61K31/555C07F15/0093C07F15/00A61P35/00
Inventor 毛宗万郑小辉谭彩萍黄华珍计亮年
Owner SUN YAT SEN UNIV
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