Preparation method and antitumor activity of a novel ruthenium complex containing 4,4'-dibromo-2,2'-bipyridine

A complex and anti-cancer activity technology, applied in 4, can solve the problems of low water solubility, high toxicity and side effects, drug resistance of cancer cells, etc., and achieve the effect of enhancing binding ability and high affinity

Active Publication Date: 2020-05-08
JIANGNAN UNIV
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  • 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 antitumor activity of a novel ruthenium complex containing 4,4'-dibromo-2,2'-bipyridine
  • Preparation method and antitumor activity of a novel ruthenium complex containing 4,4'-dibromo-2,2'-bipyridine
  • Preparation method and antitumor activity of a novel ruthenium complex containing 4,4'-dibromo-2,2'-bipyridine

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Embodiment 1

[0018] A kind of synthesis that contains 4,4'-dibromo-2,2'-bipyridine novel ruthenium complexes, comprises the following process steps:

[0019] (1) Synthesis of 4-nitrobenzoin

[0020] Put 20mL of 4-nitrobenzaldehyde and 30mL of absolute ethanol into a 250mL three-necked flask, stir, add 7mL of an aqueous solution containing 3.5g of vitamin B1 (8.75mmol), and adjust the pH of the reaction system to 8-9 with 3mol / L NaOH solution , After stirring for 1 h, let it stand at room temperature for more than 24 h. When a large amount of white solids are precipitated, filter with suction, and rinse the filter cake with deionized water three times (20 mL×3). After the solid was dried, it was recrystallized with absolute ethanol to obtain 15.4 g of white needle-like crystals with a yield of 76.9%. The reaction formula was:

[0021]

[0022] (2) Synthesis of 4-nitrobenzil

[0023] Add 2.10g of 4-nitrobenzoin (10mmol), 2.67g of N-bromosuccinimide (NBS) (15mmol) and 10mL of ethyl acet...

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Abstract

The invention provides a preparation method and antineoplastic activity of a novel ruthenium complex containing 4,4'-dibromo-2,2'-dipyridyl. The preparation method is characterized by comprising the following steps that 1, 4-nitrobenzaldehyde and vitamin B1 with the mole ratio of 22.4:1 are synthesized into an intermediate product 1; 2, the intermediate product 1 and NBS with the mole ratio of 1:1.5 are synthesized into an intermediate product 2; 3, the intermediate product 2 and 5,6-diamine-1,10-o-phenanthroline with the mole ratio of 1:1 are synthesized into an intermediate product 3; 4, ruthenium trichloride and 4,4'-dibromo-2,2'-dipyridyl with the mole ratio of 1:2 are synthesized into an intermediate product 4; 5, the intermediate product 3 and the intermediate product 4 are synthesized into the Ru(II) complex. The Ru(II) complex has planar aromatic heterocyclic ring and has quite high DNA affinity. In addition, both nitryl and bromine have the strong electrophilic effect, and the combining capacity of the complex and DNA is enhanced.

Description

technical field [0001] The invention relates to a preparation method of a novel ruthenium complex containing 4,4'-dibromo-2,2'-bipyridine, and the antitumor activity of the Ru(II) complex. 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 resistance of cancer cells, and low water solu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F15/00A61K31/555A61P35/00
Inventor 郑昌戈谢晨李明月
Owner JIANGNAN UNIV
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