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Coumarin-platinum (II) complex targeted to drug-resistant strains of lung cancer as well as synthetic method and application of coumarin-platinum (II) complex

A synthesis method and technology of coumarin derivatives are applied in the application field of coumarin-platinum complex and its synthesis, and the preparation of antitumor drugs, which can solve problems such as drug resistance, toxic and side effects, and achieve high yield , the effect of good selectivity and easy control of synthesis reaction conditions

Active Publication Date: 2019-08-23
YULIN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nowadays, metal complexes have been widely used in medical fields such as early tumor detection test strips, some clinical drugs or diagnostic reagents, but their toxic side effects and drug resistance urgently require researchers to design a high-efficiency and low-toxicity metal antineoplastic drugs

Method used

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  • Coumarin-platinum (II) complex targeted to drug-resistant strains of lung cancer as well as synthetic method and application of coumarin-platinum (II) complex
  • Coumarin-platinum (II) complex targeted to drug-resistant strains of lung cancer as well as synthetic method and application of coumarin-platinum (II) complex
  • Coumarin-platinum (II) complex targeted to drug-resistant strains of lung cancer as well as synthetic method and application of coumarin-platinum (II) complex

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Weigh 2.0mol of coumarin derivative H-QC1 and 1.0mol of dichlorobis(dimethylsulfoxide) platinum (II) in a 50.0mL autoclave, add 25.0mL of methanol, and Seal the reaction at ℃ for 24h, and obtain the reddish-brown target complex QC1-Pt. The yield was 93.4%.

Embodiment 2

[0031] Weigh 2.0mol of coumarin derivatives H-QC2 and 1.0mol of dichlorobis(dimethylsulfoxide) platinum (II) in a 50.0mL autoclave, add 35.0mL of ethanol, at 37 The reddish-brown target complex QC2-Pt was obtained after sealing reaction at ℃ for 2 hours. The yield was 80.2%.

Embodiment 3

[0033] Weigh 2.0mol of coumarin derivative H-QC2 and 1.0mol of dichlorobis(dimethylsulfoxide) platinum (II) in a 50.0mL autoclave, add 10.0mL of methanol and acetone ( v:v=13::1), and sealed reaction at 80°C for 12 hours, the reddish-brown target complex QC3-Pt was obtained. The yield was 87.5%.

[0034] The synthesis route of the coumarin-platinum (II) complex targeting human lung cancer drug-resistant strains of the present invention is as follows:

[0035]

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Abstract

The invention relates to a coumarin-platinum (II) complex targeted to drug-resistant strains of lung cancer, a synthetic method of the complex, and application of the complex in preparation of antitumor drugs. The synthetic method of the coumarin-platinum (II) complex targeted to the drug-resistant strains of lung cancer comprises the following steps: (1) adding coumarin derivatives and dichlorodimethyl sulfoxide platinum (II) into a polar solvent to obtain a mixed solution; (2) reacting the obtained mixed solution under a condition of 37-80 DEG C so as to obtain a precipitate; and (3) washingand drying the precipitate, thereby obtaining the reddish brown target product. According to the synthetic method in the invention, the coumarin derivatives serve as active ligands and are subjectedto coordination with platinum (II), and three novel coumarin-platinum (II) complexes such as QC1-Pt, QC2-Pt and QC3-Pt are produced, show excellent antitumor activity in vivo and in vitro, have potential medicinal values, and are expected to be applied to preparation of various antitumor drugs.

Description

technical field [0001] The invention relates to a platinum-based highly active complex and a synthesis method, in particular to a coumarin-platinum (II) complex targeting drug-resistant strains of lung cancer and a synthesis method thereof. The invention also relates to the application of the coumarin-platinum (II) complex targeting drug-resistant strains of lung cancer in the preparation of antitumor drugs. Background technique [0002] As early as 1978, the U.S. Food and Drug Administration approved cisplatin for the treatment of lung cancer, testicular cancer, bone cancer and early ovarian cancer. Cisplatin and other platinum complexes have had a huge impact on the treatment of cancer and are used in most anticancer chemotherapy regimens, creating a precedent for inorganic metal complexes to enter anticancer drugs. Nowadays, metal complexes have been widely used in medical fields such as early tumor detection test strips, some clinical drugs or diagnostic reagents, but t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61P35/00
CPCA61P35/00C07F15/0086
Inventor 覃其品王振凤黄小玲谭明雄苏雨婕曾嘉静罗细凤罗小玲
Owner YULIN NORMAL UNIVERSITY
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