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Water-soluble anti-cancer photosensitizer and preparation and application thereof

A photosensitizer, water-soluble technology, applied in the field of water-soluble anti-cancer photosensitizers, can solve problems such as poor water solubility, inability to kill tumors, etc., achieve low cost, low skin phototoxicity, high yield and photostability Effect

Active Publication Date: 2019-04-05
FUZHOU UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the poor water solubility of many photosensitizers, the drugs are absorbed by proteins after entering the organism and cannot be transported to the tumor tissue through the blood, so they cannot kill the tumor.

Method used

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  • Water-soluble anti-cancer photosensitizer and preparation and application thereof

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Experimental program
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Effect test

Embodiment

[0026](1) Dissolve p-aldehyde benzoic acid (1.50 g, 10.0 mmol) and 2,4-dimethylpyrrole (2.38 g, 25.0 mmol) in anhydrous tetrahydrofuran (100 mL), and add 1 drop of trifluoro Acetic acid (TFA) was reacted for 12 h in the dark. Accurately weigh a certain amount of DDQ (2.27 g, 10.0 mmol), add it into anhydrous tetrahydrofuran (50 mL) and ultrasonically shake until it is fully dissolved, then add it to the reaction solution and continue to react for 4 h, and then place it in an ice bath. Slowly add triethylamine (18 mL, 130 mmol) and boron trifluoride diethyl ether (18 mL, 149 mmol) dropwise. After the dropwise addition, continue to react overnight under dark conditions. After the reaction, filter with diatomaceous earth, wash the filtrate three times with water, saturated sodium bicarbonate solution and saturated brine successively, combine the organic layers, dry them thoroughly and then spin dry under reduced pressure. Then using dichloromethane-methanol (15:1, v / v) as eluent...

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Abstract

The invention discloses a water-soluble anticancer photosensitizer and preparation and application thereof. Firstly, mother nucleus of monocarboxyl substituted fluoroboron dipyrrol is prepared from the raw materials of carboxybenzaldehyde, 2,4-dimethyl pyrrole and the like; secondly, two heavy atomic iodines are introduced to the 2th and 6th sites to increase the oxygen quantum yield in triplet and singlet states; thirdly, the compound is further subjected to a condensation reaction with carboxybenzaldehyde, the conjugated system is expanded, the compound is absorbed and moved to a red region,and two carboxyl groups are simultaneously introduced to obtain a water-soluble fluoroboron dipyrrol anti-cancer photosensitizer. The synthetic method of this compound is simple, the raw material iseasy to obtain, the cost is low, the side reactions are few, the yield is high, the purification is easy, and the compound is conducive to industrial production.

Description

technical field [0001] The invention belongs to the field of anticancer drug design and synthesis, and in particular relates to a water-soluble anticancer photosensitizer and its preparation and application. Background technique [0002] Cancer is one of the diseases with the highest mortality rate in the world. Photodynamic therapy (PDT) is a new technology under development for the treatment of tumor and non-tumor diseases. Compared with chemotherapy, radiotherapy and other methods, photodynamic therapy has the advantages of no drug resistance, high selectivity, and less damage to normal tissues, and it can be used in combination with other mature treatment methods. Photosensitizer is a key factor affecting the effect of photodynamic therapy, which can be selectively enriched in tumor tissue, reduce damage to surrounding normal tissues, and produce ideal biological effects. At present, traditional photosensitizers such as hematoporphyrin and chlorophyll are mainly used c...

Claims

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Application Information

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IPC IPC(8): C07F5/02A61K41/00A61P35/00
CPCA61K41/0057A61P35/00C07F5/022
Inventor 刘见永杨涵周庆萌马家林
Owner FUZHOU UNIVERSITY
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