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

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...

AI Technical Summary

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 monotherapy in the field of malignant tumor diagnosis and treatment. Insensitivity of tumors and other shortcomings, realize early near-infrared fluorescence imaging diagnosis of malignant tumors, in situ photodynamic therapy and chemotherapy co-treatment and treatment process evaluation

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