Tricyclohexylphosphine-5-fluorouracil-1-yl acetic acid mononuclear silver coordination compound, preparation method and application thereof

A technology of tricyclohexylphosphine and fluorouracil, which is applied in the field of silver compounds and can solve the problem of high cytotoxicity

Active Publication Date: 2021-07-13
INST OF NEW MATERIALS & IND TECH WENZHOU UNIV
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Problems solved by technology

[0004] In view of this, the present invention provides a tricyclohexylphosphine 5-fluorouracil-1-yl acetate mononuclear silver complex to solve the problem of cytotoxicity when the me

Method used

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  • Tricyclohexylphosphine-5-fluorouracil-1-yl acetic acid mononuclear silver coordination compound, preparation method and application thereof
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  • Tricyclohexylphosphine-5-fluorouracil-1-yl acetic acid mononuclear silver coordination compound, preparation method and application thereof

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[0035] The technical solutions and technical effects of the present invention will be further described in detail below in conjunction with the accompanying drawings of the present invention.

[0036] Please see figure 1 ,, In one embodiment, a tricyclohexylphosphine 5-fluorouracil-1-yl acetate mononuclear silver complex, its chemical formula is:

[0037]

[0038] At 293K, select a 0.130mm×0.110mm×0.090mm crystal with a good shape and no cracks, fix it on the top of the glass filament with epoxy resin, and place it on a single crystal diffractometer. The Mo Kα ray is irradiated on the surface of the crystal to diffract, and the crystallographic data of the crystal are obtained by analysis.

[0039] According to the X-ray single crystal diffraction analysis results, the mononuclear silver complex belongs to the monoclinic crystal system, and the space group is P2 1 / c, the cell parameters are:

[0040]

[0041] α=90°, β=90.665(2)°, γ=90°;

[0042] Wherein, one unit c...

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Abstract

The invention provides a tricyclohexylphosphine-5-fluorouracil-1-acetic acid mononuclear silver coordination compound, a preparation method and application thereof, and belongs to the technical field of silver compounds. The mononuclear silver coordination compound is prepared by taking 5-fluorouracil-1-yl acetic acid, silver tetrafluoroborate and tricyclohexylphosphine as raw materials and reacting in the presence of triethylamine. According to the invention, one unit cell of the compound contains two same asymmetric structural units, and a central metal silver ion is respectively coordinated with a phosphorus atom in tricyclohexylphosphine and a 5-fluorouracil-1-yl acetic acid anion; researches show that the interaction mode of the mononuclear silver coordination compound and CT-DNA is an electrostatic mode, and the binding constant K of the mononuclear silver coordination compound and calf thymus DNA is 3.03*10<3> L/mol, so that the cytotoxicity is greatly reduced; and an anti-cancer activity experiment shows that the anti-cancer effect of the mononuclear silver coordination compound on MDA-MB-231 and HCT116 is remarkably enhanced compared with that of 5-fluorouracil, and particularly, the effect is better after infrared irradiation.

Description

technical field [0001] The invention belongs to the technical field of silver compounds, and in particular relates to a tricyclohexylphosphine 5-fluorouracil-1-ylacetic acid mononuclear silver complex and a preparation method and application thereof. Background technique [0002] 5-Fluorouracil can inhibit thymine nucleotide synthase, block the conversion of deoxypyrimidine nucleotides into thymine nucleotides, interfere with DNA synthesis, and also have a certain inhibitory effect on RNA synthesis. It is clinically used to relieve or inhibit colon Cancer, rectal cancer, gastric cancer, breast cancer, liver cancer, etc. However, 5-fluorouracil has relatively serious toxic and side effects, which can cause gastrointestinal discomfort and damage the nervous system. In severe cases, it can cause cerebral palsy and cerebellar degeneration. [0003] Studies have shown that 5-fluorouracil derivatives can improve the anticancer activity of 5-fluorouracil and reduce its toxic and s...

Claims

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Application Information

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IPC IPC(8): C07F1/10A61P35/00
CPCC07F1/10A61P35/00
Inventor 郑勉虹高兰星
Owner INST OF NEW MATERIALS & IND TECH WENZHOU UNIV
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