Preparation method and antineoplastic activity of novel Ru(II) complex containing 4-nitrobenzene

A technology of anti-tumor activity and complexes, applied in the field of anti-tumor activity, can solve the problems of low water solubility, high toxicity and side effects, drug resistance of cancer cells, etc., and achieve the effect of enhanced binding ability and high affinity

Inactive Publication Date: 2016-08-24
JIANGNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Drugs such as cisplatin have problems such as high toxicity and side effects and drug resistance of cancer cells, and their water solubility is small

Method used

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  • Preparation method and antineoplastic activity of novel Ru(II) complex containing 4-nitrobenzene
  • Preparation method and antineoplastic activity of novel Ru(II) complex containing 4-nitrobenzene
  • Preparation method and antineoplastic activity of novel Ru(II) complex containing 4-nitrobenzene

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Embodiment 1

[0020] A kind of synthesis that contains 2,3-two (4-nitrophenyl) pyrazine [2,3-f] [1,10] phenanthroline novel Ru (II) complexes, comprises the following process steps:

[0021] (1) Synthesis of 5,6-diketone-1,10-phenanthroline

[0022] Add 10g1,10-phenanthroline (55.6mmol) in a 250mL three-necked flask, quickly add 60mL of concentrated sulfuric acid under ice-salt bath conditions, quickly add 13.2g KBr (111mmol) after dissolving, slowly add 30mL of concentrated nitric acid dropwise, and heat up to React at 110°C for 2.5 hours. After the reaction is completed, cool to room temperature. Pour the reaction solution into 500 g of crushed ice and neutralize it with 10 mol / L NaOH solution. A large amount of yellow solid precipitates, which is filtered by suction, washed with a large amount of distilled water, and recrystallized from ethanol to obtain a yellow color. Needle crystals were suction filtered and dried in vacuo to obtain 7.17 g of solid, with a yield of 60.8%. The reactio...

Embodiment example 2

[0036] Implementation Case 2: Anti-tumor activity experiment of Ru(II) complexes

[0037]The invention adopts the MTT method to measure the toxicity of Ru(II) complexes on tumor cells in vitro, and takes liver cancer cell line Hep G2 and human melanoma cell line F10-B16 as detection objects. The cultured cancer cell suspension was inoculated into a clean 96-well culture plate, 200 μL / well, and the obtained Ru(II) complex was added to the cell culture plate in a concentration gradient (6.25 μM-100 μM), and each Well 100 μL, the concentration of each Ru(II) complex is 2 parallel plates, no Ru(II) complex is added to the blank control group, only the culture solution is added. Place in a 37°C incubator at a constant temperature for 48 hours, add 20 μL of 5 g / L MTT to each well, continue to incubate for 5 hours, then add 100 μL of SDS to each well, and measure the absorbance value of each well at a wavelength of 570 nm on a microplate reader after 10 hours. The inhibition rate wa...

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Abstract

The invention provides a novel Ru(II) complex containing 2,3-bis(4-nitrophenyl)pyrazine[2,3-f][1,10] phenanthroline with antineoplastic activity and a preparation method thereof. The preparation method is characterized by comprising the following steps that 1, 1,10-o-phenanthroline and potassium bromide react to synthesize an intermediate product 1 according to the mole ratio of 1:2; 2, the intermediate product 1, hydroxylamine hydrochloride and sodium carbonate are synthesized into an intermediate product 2 according to the mole ratio of 1:3.5:1.5; 3, the intermediate product 2 and sodium dithionite are synthesized into an intermediate product 3 according to the mole ratio of 1:5; 4, the intermediate product 3 and 4'4-dinitrobenzil are synthesized into an intermediate product 4 according to the mole ratio of 1:1; 5, the intermediate product 4 and cis-bis-(2,2'-bipyridine)dichlororuthenium(II) dihydrate are synthesized into the Ru(II) complex according to the mole ratio of 1:1.3. The Ru(II) complex has planar aromatic heterocycle and has quite high DNA affinity, nitryl has the strong electrophilic effect, and the combining capacity of the complex and DNA is enhanced.

Description

technical field [0001] The present invention relates to a preparation method of a novel Ru(II) complex containing 2,3-bis(4-nitrophenyl)pyrazine[2,3-f][1,10]phenanthroline, and the obtained Antitumor activity of Ru(II) complexes. Background technique [0002] Metal complexes interact with DNA through electrostatic binding, channel binding, and insertion binding. Among them, the insertion combination method is the best, because the insertion into the base pair of DNA can directly damage the base pair and affect the DNA replication of cancer cells. If the metal complex can recognize the gene mutation site of cancer cells, insert into the mismatched base pair, and prevent its replication, it can be used as a good anticancer drug to treat genetic diseases fundamentally. [0003] In 1969, cisplatin was first reported to have anti-tumor activity, and was subsequently used in clinical trials. Drugs such as cisplatin have problems such as high toxicity and side effects, drug resi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61P35/00
Inventor 郑昌戈谢晨李明月
Owner JIANGNAN UNIV
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