Synthesis method of light controlled-release compound and application of light controlled-release compound in tumor treatment
A synthesis method and compound technology, applied in the field of photo-controlled release compound synthesis, can solve the problems of tumor insensitivity, poor diagnosis and treatment effect, single imaging and treatment mode, etc., and achieve the effect of improving curative effect.
Inactive Publication Date: 2020-08-21
ZUNYI MEDICAL UNIVERSITY
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[0006] What the present invention is to solve is to meet the needs of the existing clinical and future individualized medical treatment with targeted drugs and multiple therapy combination drugs to overcome the current problems in the field of malignant tumor diagnosis and treatment, such as single imaging and treatment mode, poor diagnosis and treatment effect, and the effect of single therapy on tumor Insensitivity and other disadvantages, realize the technical problem of light-controlled release of in situ chemotherapeutic drugs for malignant tumors and synergistic treatment of photodynamic therapy and chemotherapy
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[0032] The content of the present invention will be described in detail below in conjunction with specific embodiments. It should be noted that what follows is an explanation rather than a limitation of the present invention.
[0033] 1. The synthetic method of the light-controlled release compound of the present invention;
[0034]Including the following steps: (i) 4-benzoyl chloride (2mmol) was dissolved in a round-bottomed flask containing 100mL of dichloromethane, and argon was introduced into the round-bottomed flask for 15min, and 2,4-dimethyl- 4mmol of 3-ethyl-1H-pyrrole, then a small amount of trifluoroacetic acid was added dropwise, the mixture was stirred at room temperature for about 12h, 4mmol of 2,3-dichloro-5,6-dicyano-1,4-benzoquinone was added, After continuing to stir for 4h, add 10mmol of triethylamine and continue to stir for 15min. Slowly add 15mmol of boron trifluoride ether in an ice bath. After the dropwise completion, the mixture is stirred overnight a...
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Abstract
The invention relates to a synthesis method of a light controlled-release compound. The above lead compound is composed of a BODIPY parent nucleus and chlorambucil, and light controlled-release drug,photodynamic therapy and chemotherapy are integrated in the same molecular structure. The invention also discloses an application of the compound in tumor treatment. The lead compound is simple in structure and small in molecular weight, has a determined chemical structure, is easy to prepare, purify and further modify, and has the remarkable characteristics of low toxicity to mice and the like, so that the basic requirements of clinical medication are met. Proved by in-vitro and in-vivo experiments, the lead compound has an accurate controlled-release chemotherapeutic drug chlorambucil undervisible light radiation, and the optical radiation time and the drug release amount are in a positive correlation relationship, so that the chemotherapeutic drug and singlet oxygen are accurately released by a single molecule through optical stimulation, and the synergistic treatment of chemotherapy/photodynamic therapy of living tumors is realized. Therefore, the lead compound for photodynamic therapy cooperated with photocontrolled-release chemotherapy has a good application prospect in the aspect of tumor therapy.
Description
technical field [0001] The invention relates to a synthesis method of a light-controlled release compound and its application in tumor treatment, belonging to the field of pharmaceutical and chemical synthesis. Background technique [0002] At present, cancer has become one of the major diseases threatening human health. Therefore, the effective prevention and treatment of cancer has always been an important topic in the field of medical research. Currently, clinical treatments for tumors include chemotherapy, surgery, photodynamic therapy, and radiotherapy [Zhou J, Yu G, Huang F. Chemical Society Reviews, 2017, 46: 7021-7053]. Among these treatment options, chemotherapy is currently the mainstay of clinical cancer treatment. However, single chemotherapy drugs cannot meet the clinical treatment requirements due to low bioavailability, high toxicity and side effects, and easy multidrug resistance, especially in the late stage of tumor or metastasis. Therefore, combination t...
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IPC IPC(8): C07F5/02C09K11/06A61K41/00A61K31/196A61P35/00
CPCC07F5/022C09K11/06A61K41/0057A61K31/196A61P35/00C09K2211/1055
Inventor 高杰袁泽利曹亚萍
Owner ZUNYI MEDICAL UNIVERSITY
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