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A pt(iv) anticancer drug with mixed axial ligands and its preparation method

A ligand and axial technology, applied in anti-tumor drugs, drug combinations, chemical instruments and methods, etc., can solve the problem of low pharmacological activity of satraplatin, avoid strong toxic and side effects, improve reactivity, and enhance positive electrical effect

Active Publication Date: 2016-02-10
于迎涛
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Problems solved by technology

[0011] The purpose of the present invention is to solve the problem of the low pharmacological activity of the existing Pt (IV) clinical anticancer drug Satraplatin, and propose a new Pt (IV) class anticancer drug structure design and preparation method with mixed axial ligands

Method used

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  • A pt(iv) anticancer drug with mixed axial ligands and its preparation method
  • A pt(iv) anticancer drug with mixed axial ligands and its preparation method
  • A pt(iv) anticancer drug with mixed axial ligands and its preparation method

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Embodiment 1

[0060] The preparation condition control of the platinum-based anticancer drug with mixed axial ligands in the present invention is based on the following methods:

[0061] (1) Prepare a saturate platinum saturated aqueous solution in the dark and at room temperature, and measure its ultraviolet-visible absorption spectrum. The test instrument is JASCO550 UV-Vis absorption spectrometer. Such as Figure 5 As shown, when the wavelength is less than 450nm, the absorption of incident light is detected, and as the wavelength of incident light decreases, the absorption intensity gradually increases; when the wavelength of incident light is greater than 450nm, Saite platinum aqueous solution has no obvious absorption of incident light , indicating that the upper wavelength limit of the irradiated light to excite the d–d transition of satyr platinum is 450 nm.

[0062] (2) Prepared by irradiation with purple light (415nm, half width 12nm), blue light (477nm, half width 22nm), green ...

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Abstract

The invention discloses a Pt (IV) type anti-cancer medicine with mixed axial ligands and a preparation method thereof. The Pt (IV) type anti-cancer medicine with the mixed axial ligands has an octahedral coordination structure which is composed of two pairs of planar ligands and one pair of mixed axial ligands bonded with Pt<4+>, one of the axial ligands is a ligand having a relatively strong bonding effect with the Pt<4+>, and the other one is a ligand having a relatively weak bonding effect with the Pt<4+>. By adopting the design of strong effect and weak effect collocation, the medicine can be relatively easily reduced into a Pt (II) species and has a relatively high pharmacological activity in comparison with the existing Pt (IV) medicine satraplatin. The embodiment proves that in comparison with the satraplatin, the medicine can more easily generate a product of bonding between Pt and an N7-bit bond of guanine in a photophobic reaction system in which ascorbic acid, reduced glutathione and DNA (Deoxyribonucleic Acid) mode species 5'-dGMP (Deoxyguanylic Acid) coexist, and has wide application prospect for achieving a high-efficiency and low-toxicity anti-cancer goal.

Description

technical field [0001] The invention belongs to the field of chemical synthesis of new drugs, and relates to a Pt (IV) anticancer drug with mixed axial ligands and a preparation method thereof. Background technique [0002] Cancer poses a great threat to human health, and the research on anticancer drugs has been widely concerned. The target molecule of platinum-based anticancer drugs is deoxyribonucleic acid (DNA) in cells. After the Pt in the platinum-based drug is bonded to the N7 atom of guanine in DNA, it can inhibit DNA replication and induce cell apoptosis, thereby achieving anti-cancer effects. Platinum-based anticancer drugs are not only more sensitive to many rapidly proliferating cancer cells than normal cells, but also have a greater effect on rapidly dividing normal cells (bone marrow cells, hair follicles, and epithelial cells), which can cause varying degrees of toxic and side effects. [0003] The design of platinum-based anticancer drugs usually follows th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/282A61P35/00C07F15/00
Inventor 于迎涛
Owner 于迎涛
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