Preparation method and application of 5-fluorouracil-1-yl acetic acid phenanthroline copper tetrafluoroborate anticancer functional complex

A technology of roline copper tetrafluoroborate and phenanthrene acetate, which is applied in the field of copper complexes, can solve the problems of DNA irreversibility and blockage, and achieve good anti-tumor activity

Inactive Publication Date: 2020-11-24
INST OF NEW MATERIALS & IND TECH WENZHOU UNIV
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Problems solved by technology

At present, the mechanism of action of many anticancer drugs is through the mode of covalent binding to DNA, which can be observed through several binding s

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  • Preparation method and application of 5-fluorouracil-1-yl acetic acid phenanthroline copper tetrafluoroborate anticancer functional complex
  • Preparation method and application of 5-fluorouracil-1-yl acetic acid phenanthroline copper tetrafluoroborate anticancer functional complex
  • Preparation method and application of 5-fluorouracil-1-yl acetic acid phenanthroline copper tetrafluoroborate anticancer functional complex

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[0030] The present invention is further described below through specific examples, but the present invention is not limited only to the following examples. Within the scope of the present invention or without departing from the content, spirit and scope of the present invention, changes, combinations or substitutions to the present invention are obvious to those skilled in the art and are included in the scope of the present invention Inside.

[0031] Preparation method and application of 5-fluorouracil-1-ylacetic acid o-phenanthroline copper tetrafluoroborate anticancer functional complex, wherein 5-fluorouracil-1-ylacetic acid has the following characteristics, and the yield is 89.46%. Melting point: 279.7-280.5°C. Elemental analysis (%): C, 38.11; H, 2.74; N, 14.36. Theoretical (%): C, 38.26; H, 2.66; N, 14.88. 1 H NMR (500MHz, DMSO) δ13.20(s, 1H, COOH), 11.93(d, 1H, NH, J=5.0), 8.08(d, 1H, OCCH, J=10.0), 4.37(s, 2H, CH 2 ) ppm. 13 C NMR (126 MHz, DMSO) δ: 169.18, 157...

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Abstract

The invention discloses a preparation method and application of a 5-fluorouracil-1-yl acetic acid phenanthroline copper tetrafluoroborate anticancer functional complex. The invention provides a synthesis method of a novel Cu complex [Cu(phen)2L1]BF4.H2O (phen=1,10-phenanthroline, L1=5-fluorouracil-1-yl acetic acid), and the synthesis method is used for characterization. A crystal structure of thecomplex is analyzed through an X-ray diffraction single crystal structure and a differential thermal analysis method, and the result shows that the complex has certain stability at the environment temperature. The combination of the complex and CT-DNA is studied through ultraviolet-visible absorption spectrometry, fluorescence spectrometry and electrochemical methods, and results show that the complex and DNA have electrostatic interaction. In addition, in an in-vitro cell experiment, the complex [Cu(phen)2L1]BF4.H2O can well inhibit the growth of human breast cancer cells and human colon cancer cells. The complex [Cu(phen)2L1]BF4.H2O can be listed as a promising anti-tumor candidate drug on the basis that structural modification is conducted through biologically friendly metal copper andgood anti-tumor activity is shown.

Description

technical field [0001] The invention relates to the field of copper complexes, in particular to a preparation method and application of a 5-fluorouracil-1-ylacetic acid o-phenanthroline copper tetrafluoroborate anticancer functional complex. Background technique [0002] Cancer is a general term for a large group of diseases involving the uncontrolled growth of abnormal cells that may invade or spread to other parts of the body. It is a ubiquitous and recurrent disease that threatens human health at all times. As early as the 50s of the last century, 5-fluorouracil (5-FU) was successfully used in the clinical application of cancer treatment, which opened up a new stage of anti-metabolism tumor treatment drugs, and became a clinically used drug for the treatment of gastric cancer, pancreatic cancer and colorectal cancer. , head and neck tumors, etc., is one of the main anticancer drugs. [0003] However, due to the significant first-pass metabolism of 5-FU, low bioavailabili...

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Application Information

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IPC IPC(8): C07F1/08A61P35/00
CPCC07F1/005A61P35/00C07B2200/13
Inventor 吴东林何华成郑勉虹奚云红胡茂林
Owner INST OF NEW MATERIALS & IND TECH WENZHOU UNIV
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