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A kind of medicine for treating cancer, its synthesis method and application

A cancer and drug technology, which is applied in its synthesis and the field of cancer treatment drugs, can solve problems affecting drug application and patient pain, and achieve the effects of inhibiting cancer cell proliferation, reducing biological toxicity, and reducing damage

Active Publication Date: 2022-04-08
河北艾克美冀生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its severe bone marrow suppression, heart, liver, kidney and other toxic and side effects have seriously affected the clinical application of the drug and caused pain for patients.

Method used

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  • A kind of medicine for treating cancer, its synthesis method and application
  • A kind of medicine for treating cancer, its synthesis method and application
  • A kind of medicine for treating cancer, its synthesis method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 A drug for treating cancer (compound 4708SP-1)

[0038] This example is compound 4708SP-1, which is mainly composed of a DNA fragment and paclitaxel. The DNA fragment can be directly taken up by cancer cells without packaging and rarely enters normal cells. The DNA fragment contains 50 bases, and its nucleoside The acid sequence is:

[0039] 5'-CATTCTCTGATGACAAGTTCATTTTCCATAAGGATCTGTGCCAAGCTCAG-3'

[0040] The above nucleotide sequences are artificially synthesized sequences or selected from human cell genomic DNA.

[0041] The chemical name of paclitaxel in this example is 5β,20-epoxy-1,2α,4,7β,10β,13α-hexahydroxytaxane-11-en-9-one-4,10-diacetate -2-Benzoate-13[(2'R,3'S)-N-benzoyl-3-phenylisoserine].

[0042] The usage and dosage of this embodiment are: intravenous injection, transcatheter arterial injection dosage is 100 ~ 500mg / m 2 .

Embodiment 2

[0043] Implementation 2 DNA fragment screening process

[0044] AFP gene is highly expressed in liver cancer, so the DNA fragment screening in the present invention is related to AFP gene. Different sequences of its genes are labeled with fluorescein to detect its targeting by cancer cells and normal cells. The specific method is as follows:

[0045] The fluorescence in situ hybridization kit (FISH) used in the experiment was purchased from Mirus Company in the United States, and the operation method was carried out in accordance with the kit instructions. After the screened DNA fragments were amplified by PCR, they were purified by phenol chloroform and adjusted to 1 g / L. Fluorescein Rhodamine was added to the DNA fragment, incubated at 37°C for 1 h; then purified with G50 gel column. The fluorescently labeled DNA fragments were added to the cell culture medium, incubated at 37°C for 16 hours, washed with PBS, and fixed with 4% formalin. Then use the same method to double...

Embodiment 3

[0046] Example 3 Synthesis method of drug for treating cancer (compound 4708SP-1)

[0047] This embodiment provides two synthesis methods for a drug for treating cancer provided in Example 1, specifically as follows:

[0048] 1. The first synthetic method

[0049] The synthetic route of the first synthetic method is:

[0050] (1) A phosphodiester bond on the nucleotide sequence of the DNA fragment is modified by phosphorothioate into a phosphorothioate bond to generate compound 1, and compound 1 is covalently bonded to the carbon end of n-hexylamine to form compound 2; reaction Formula is

[0051]

[0052] (2) Paclitaxel reacts with succinic anhydride to generate compound 3, N,N-dicyclohexylcarbodiimide (DCC) and N-hydroxysuccinimide (NHS) activate the carboxyl group of compound 3 to generate compound 4 ; The reaction formula is

[0053]

[0054] 3) Compound 4 is covalently combined with the amino group of compound 2 to generate compound 4708SP-1, the reaction formula ...

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Abstract

The invention discloses a drug for treating cancer, its synthesis method and application. The drug is mainly composed of a DNA fragment and paclitaxel; the synthesis method of the drug is as follows: firstly, the DNA fragment is modified by phosphorothioate, and then co-modified with the carbon terminal of n-hexylamine. combined with modified paclitaxel to generate compound 4708SP‑1; the drug is used to treat primary cancer and / or metastatic cancer such as advanced liver cancer. The DNA fragment in the medicine of the present invention can be directly taken up by cancer cells without packaging and rarely enters normal cells, which simplifies the synthesis steps and reduces the damage of the medicine to normal tissues, and is used for treating advanced cancer such as advanced liver cancer.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a medicine for treating cancer, its synthesis method and application. Background technique [0002] In medicine, cancer refers to a malignant tumor originating from epithelial tissue, which has biological characteristics such as abnormal cell differentiation and proliferation, uncontrolled growth, invasion and metastasis, and is a kind of chronic disease with relatively high difficulty in treatment. The number one cause of death among urban and rural residents. [0003] The current cancer treatment methods include surgery, chemotherapy, radiotherapy, etc., but there are certain defects. For example, although surgery is the best treatment for early cancer, early diagnosis of cancer is difficult. Many patients have entered the middle and late stages of cancer when they are diagnosed, and surgery has failed; chemotherapy is the use of cytotoxic drugs that inhi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H21/04C07H1/00A61P35/00
Inventor 孔彦平刘锦红
Owner 河北艾克美冀生物科技有限公司
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