Preparation method and application of tumor-targeted diagnosis and treatment combined single-molecule lead compound

A lead compound and tumor-targeting technology, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, antineoplastic drugs, etc., can solve tumor insensitivity, poor diagnosis and treatment effect, imaging and treatment mode Single and other problems, to achieve the effect of improving curative effect

Inactive Publication Date: 2019-06-04
ZUNYI MEDICAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0007] The main technical problem to be solved by the present invention is to address the current clinical needs of targeted drugs and combination drugs for diagnosis and treatment in order to overcome the single imaging and treatment mode, poor diagnosis and treatment effect, and mon

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  • Preparation method and application of tumor-targeted diagnosis and treatment combined single-molecule lead compound
  • Preparation method and application of tumor-targeted diagnosis and treatment combined single-molecule lead compound
  • Preparation method and application of tumor-targeted diagnosis and treatment combined single-molecule lead compound

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Embodiment Construction

[0049] 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.

[0050] 1. Synthesis of the lead compound for single-molecule multifunctional diagnosis and treatment of the present invention:

[0051] The synthesis route of the lead compound used in combination with single molecule multifunctional diagnosis and treatment of the present invention is as follows: figure 1 As shown, the synthesis method mainly refers to the literature (i: Chunyan Wang, Keith Man-Chung Wong. Selective Hg 2+ Sensing Behaviors of Rhodamine Derivatives with Extended Conjugation Based on TwoSuccessive Ring-Opening Processes[J].Inorg.Chem.,2013,52,13432-13441; ii: KeyinLiu, Huiming Shang, Xiuqi Kong, et al.A novel near-infrared fluorescent probe for H2O2in alkaline environment and the application for H 2 o 2 imaging in vitro and in vivo[J]...

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Abstract

The invention discloses a preparation method and application of a tumor-targeted diagnosis and treatment combined single-molecule lead compound, and the lead compound is prepared from a terpene-mothernucleus, aryl nitrogen mustardand N, N-diethyl tertiary nitrogen, wherein the structure is shown in (I) as shown in the specification, and mitochondria targeting, fluorescence imaging diagnosis, photodynamic therapy and chemotherapy are integrated in the same molecular structure. The lead compound has the prominent characteristics of being simple in structure and small in molecular weight, determined in chemical structure, easy to prepare, purify and further modify, low in the toxicity to mice, and the like, and the basic requirements of clinical medication are met. An in-vitro experiment proves that tertiary amine electropositivity and amitochondrial electronegativity found by near infrared fluorescence imaging of the lead compound structure remarkably target tumor cells and tumor tissues, photodynamic therapy effects can be generated under near-infrared radiation, and the tertiary amine electropositivity and amitochondrial electronegativity and the nitrogen mustard in the lead compound structure can generate chemical treatment and synergistic treatment, so that the growth of tumors can be remarkably inhibited.

Description

technical field [0001] The invention relates to a preparation method and application of a monomolecular lead compound for tumor-targeted diagnosis and treatment, and belongs to the field of biomedicine. Background technique [0002] Malignant tumors are common and frequently-occurring diseases that seriously threaten human health, and there are currently no satisfactory prevention and treatment measures. Although clinical techniques for tumor diagnosis and treatment are increasing and methods are constantly being updated, tumor treatment is increasingly becoming a "protracted battle", which brings a huge economic burden and ideological burden to tumor patients. Therefore, as the fastest-growing and most important drug chemotherapy in clinical tumor treatment, how to develop efficient, safe and economical diagnosis and treatment that integrates targeted and accurate tumor diagnosis, grading, prognosis evaluation and treatment from the perspective of molecular design Combinat...

Claims

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Application Information

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IPC IPC(8): C07D493/10A61K41/00A61K47/55A61K49/00A61P35/00
Inventor 袁泽利屈小芳麦宇涵袁付明高健美李晓飞
Owner ZUNYI MEDICAL UNIVERSITY
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