Cisplatin-flurbiprofen prodrug, as well as preparation method and application thereof

A flurbiprofen and cisplatin technology, applied in the field of chemical prodrugs and their preparation, can solve the problems of not reversing drug resistance, unable to more effectively improve drug treatment effect, etc., and achieve the effect of enhancing anti-tumor effect
CN107445818AActive Publication Date: 2017-12-08THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
Publication Date
2017-12-08

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Abstract

The invention provides a cisplatin-flurbiprofen prodrug, as well as a preparation method and application thereof. The cisplatin-flurbiprofen prodrug is a tetravalent platinum prodrug, and an anti-inflammatory drug flurbiprofen is connected to the two axial positions of tetravalent platinum. The preparation method of the cisplatin-flurbiprofen prodrug comprises the following steps: (1) enabling the flurbiprofen to react with oxalyl chloride to obtain flurbilofenyl chloride; (2) enabling the flurbilofenyl chloride to react with dihydroxyl diamineplatinum dichloride to obtain the cisplatin-flurbiprofen prodrug. The prepared cisplatin-flurbiprofen prodrug can be reduced by a reducing molecular such as glutathione in a cell in a cellular environment to release monomolecular cisplatin and bimolecular flurbiprofen, DNAs (deoxyribonucleic acids) are damaged by the cisplatin, the flurbiprofen has an anti-inflammatory effect, and the cisplatin and the flurbiprofen are simultaneously released at the same position in the cell in a prodrug connecting manner to reverse the drug resistance of tumor cells to the cisplatin, thereby synergistically killing tumors and enhancing an anti-tumor effect.
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Description

technical field

[0001] The invention belongs to the field of medicinal chemistry and relates to a chemical prodrug and its preparation method and application. Background technique

[0002] As a representative drug in the field of inorganic medicinal chemistry, cisplatin has been used in the clinical trials of various solid tumors such as ovarian cancer, testicular cancer, bladder cancer, and lung cancer since it was approved for use by the US Food and Drug Administration (FDA) in 1978. First-line chemotherapy is one of the most widely used broad-spectrum anticancer drugs in clinical practice. Its mechanism of action is: after cisplatin enters the cell and is activated, it binds to DNA in the nucleus to form an adduct, inhibits the transcription and replication of DNA, and induces apoptosis. Cisplatin is effective, but its disadvantages are also obvious, such as dose-limiting toxicity (ototoxicity, nephrotoxicity, neurotoxicity, bone marrow suppression, etc.), severe gastroi...

Claims

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