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A kind of polypyridine ruthenium complex and its preparation method and application

A complex, ruthenium pyridine technology, which is applied in the direction of pharmaceutical formulations, chemical instruments and methods, medical preparations containing active ingredients, etc., can solve the problems of high dark toxicity and low phototoxicity, and achieve low dark toxicity, high phototoxicity, The effect of maintaining anticancer activity

Active Publication Date: 2021-05-14
TECHNICAL INST OF PHYSICS & CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, currently reported ruthenium photoactivated chemotherapeutic drugs have disadvantages such as low phototoxicity or high dark toxicity.

Method used

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  • A kind of polypyridine ruthenium complex and its preparation method and application
  • A kind of polypyridine ruthenium complex and its preparation method and application
  • A kind of polypyridine ruthenium complex and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] The preparation method of polypyridine ruthenium complex, comprises the steps:

[0035] Reflux 210mg (1mmol) of 4,5-difluoro-1,2-phenylenediamine with 126mg (1mmol) of 1,10-o-phenanthrene-5,6-dione in ethanol for three hours and dissolve in ethanol 11,12-difluorobipyrido[3,2-a:2',3'-c]phenazine was obtained by recrystallization. Then 90mg (0.3mmol) of 11,12-difluorobipyrido[3,2-a:2',3'-c]phenazine was dimerized with 75mg (0.15mmol) of dichlorophenylruthenium(II) The solid was stirred overnight in 40 mL of methanol until a clear red liquid was formed, then the solvent was removed and redissolved in 40 mL of water. Add 1 mL of excess pyridine, degas with nitrogen for 30 minutes, heat to reflux for 2 hours and turn on nitrogen to cool. The product was eluted and purified on a silica gel chromatography column with acetonitrile: saturated aqueous potassium chloride solution = 10:1, and the excess potassium chloride in the column product was removed by utilizing the low sol...

Embodiment 2

[0039] Repeat Example 1, the difference is that after the purification is completed, add NH 4 PF 6 or NaClO 4 , the monovalent anion obtained by ion exchange is (PF 6 ) - or (ClO 4 ) - A polypyridine ruthenium complex having the structure described in formula I.

Embodiment 3

[0041] Antitumor activity experiments and results of the prepared complexes.

[0042] Cells and culture conditions: HeLa (human cervical cancer cell line), SKOV-3 (human ovarian cancer cell line), SKOV-3-ddp (human ovarian cancer cell line cisplatin-resistant cell line), provided by Cancer Hospital, Chinese Academy of Medical Sciences supply. Cells were cultured in DMEM medium supplemented with 10% fetal bovine serum and 100 units of penicillin and streptomycin.

[0043] Cytotoxicity Test:

[0044]The cytotoxicity of the complexes was determined by the classical MTT method. Cells were planted on a 96-well plate at a density of 5,000-10,000 cells / well, cultured for 24 hours at 37°C in an environment of 5% carbon dioxide, and then cultured with complexes prepared in Example 1 containing different concentration gradients. 4 hours, at (470nm, 22.5mW / cm 2 ) light intensity for 20 minutes, and then continue to cultivate for 20 hours. After adding 5 mg / ml of MTT (thiazolium blue...

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Abstract

The invention discloses a polypyridine ruthenium complex, which has the structure described in the following formula I: wherein, X ‑ Represents a charge-balancing monovalent anion. The complex has high phototoxicity and low dark toxicity, can be preferably used in the preparation of photoactivated antitumor drugs, and can overcome the defect of large toxic and side effects of traditional chemotherapy drugs. The invention also discloses the preparation method and application of the polypyridine ruthenium complex.

Description

technical field [0001] The invention relates to the field of antitumor drugs, in particular to the field of photoactivated antitumor drugs. More specifically, it relates to a polypyridine ruthenium complex and its preparation method and application. Background technique [0002] Although platinum-based chemotherapeutic drugs represented by cisplatin are widely used clinically, their disadvantages such as high toxicity and side effects and drug resistance of tumor cells limit their clinical therapeutic effect. Therefore, actively seeking new non-platinum anti-tumor drugs and new tumor treatment methods is an important direction of current drug research and development. [0003] Photoactivated chemotherapy (PACT) is a new type of tumor treatment method, that is, by designing and synthesizing prodrug molecules that are inactive under dark conditions, the prodrugs can be converted into active drug molecules under light conditions. Using the controllability of light in time and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F15/00A61P35/00A61K31/555A61K41/00A61K33/243
Inventor 程学新热娜·博尔汗周前雄王雪松
Owner TECHNICAL INST OF PHYSICS & CHEMISTRY - CHINESE ACAD OF SCI
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