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Novel 2-phenylpyridine-platinum (IV) precursor anti-cancer complex as well as synthesis method and application thereof

A technology of phenylpyridines and synthetic methods, which is applied in the field of pyridine-platinum complexes and synthesis, can solve the problems of low biopharmaceutical efficiency, high toxicity and side effects, and inability to take orally, and achieves simple synthetic routes, simple structures, and high yield. high rate effect

Active Publication Date: 2019-10-15
YULIN NORMAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] Cisplatin-based chemotherapeutic drugs have been widely used in the treatment of various types of cancer in clinical practice; however, the existing bivalent platinum-based chemotherapeutic drugs have many disadvantages such as high toxicity and side effects, low biopharmaceutical efficiency, drug resistance, and inability to take orally.

Method used

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  • Novel 2-phenylpyridine-platinum (IV) precursor anti-cancer complex as well as synthesis method and application thereof
  • Novel 2-phenylpyridine-platinum (IV) precursor anti-cancer complex as well as synthesis method and application thereof
  • Novel 2-phenylpyridine-platinum (IV) precursor anti-cancer complex as well as synthesis method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027] Weigh 2.0mmol of 2-phenylpyridine (H-PPy) and 1.0mmol of metal salt K 2 PtCl 6 , placed in a 100mL round bottom flask, dissolved in a mixed solution of 25.00mL methanol and dichloromethane (25:1), reacted at 55°C for 6h, filtered the reaction solution, washed, and dried at 40°C. That is, the yellow target product Pt1 was obtained. The yield was 85.6%.

Embodiment 2

[0029] Weigh 2.0mmol of 2-phenylpyridine (H-PPy) or 2-[4-(trifluoromethyl)phenyl]pyridine (H-TFPy) and 1.0mmol of metal salt K 2 PtCl 6 , placed in a 100mL round-bottomed flask, dissolved in 55.0mL of a mixed solution of methanol and dichloromethane (100:1), reacted at 75°C for 72h, filtered the reaction solution, washed, and dried at 45°C. That is, the yellow target product Pt2 was obtained.

Embodiment 3

[0031] Weigh 2.0mmol of 2-phenylpyridine (H-PPy) and 1.0mmol of metal salt K 2 PtCl 6 , placed in a 100mL round bottom flask, dissolved in a mixed solution of 10.00mL methanol and dichloromethane (50:1), reacted at 30°C for 24h, filtered the reaction solution, washed, and dried at 40°C. That is, the yellow target product Pt1 was obtained. The yield was 70.8%.

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Abstract

The invention relates to a novel 2-phenylpyridine-platinum (IV) precursor anti-cancer complex as well as a synthesis method and the application of the complex in preparing anti-tumor medicines, relates to a phenylpyridine-platinum complex and aims to obtain an efficient and low-toxicity anti-cancer substance. The novel 2-phenylpyridine-platinum (IV) precursor anti-cancer complex has structural formulae as shown in Pt1 and Pt2. The synthesis method of the complex comprises the following steps: dissolving ligand 2-phenylpyridine-H-PPy or 2-[4-(trifluoromethyl) phenyl] pyridine H-TFPy and a metallic salt K2PtCl6 into a mixed solution of methanol and dichloromethane, and carrying out a coordination reaction, so as to obtain a yellow target product, namely a 2-phenylpyridine-platinum (IV) precursor anti-cancer complex Pt1 or Pt2. The two 2-phenylpyridine-platinum (IV) precursor anti-cancer complexes Pt1 and Pt2 provided by the invention show remarkable in-vitro anti-tumor activity and toxicity selectivity as a whole, in addition are cheap in raw materials, convenient in synthesis and economic, have good potential medicine values and have the potential of being applied to preparation ofvarious anti-tumor medicines.

Description

technical field [0001] The invention relates to a pyridine-platinum complex and a synthesis method, in particular to a novel 2-phenylpyridine-platinum (IV) precursor anticancer complex and a synthesis method thereof. The invention also relates to the application of the novel 2-phenylpyridine-platinum (IV) precursor anticancer complex in the preparation of antitumor drugs. Background technique [0002] Cisplatin-based chemotherapeutic drugs have been widely used in the treatment of various types of cancer in clinical practice; however, the existing bivalent platinum-based chemotherapeutic drugs have many disadvantages such as high toxicity and side effects, low biopharmaceutical efficiency, drug resistance, and inability to take orally. . Therefore, the development of new platinum-containing anticancer agents with better activity, lower toxicity, and ability to overcome drug resistance has always been an urgent research topic in this field. Among them, tetravalent platinum p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61P35/00A61K31/555
CPCC07F15/0086A61P35/00C07B2200/13
Inventor 谭明雄覃其品孙凌杰王振凤林李梅
Owner YULIN NORMAL UNIVERSITY
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