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Dimer prodrug and preparation method and application thereof

A technology of dimer and prodrug, which is applied in the field of dimer prodrug and its preparation, can solve the problems of observing the activation of prodrug, achieve the effect of enhancing treatment, reducing toxicity and enhancing therapeutic effect

Active Publication Date: 2020-12-11
SOUTH CHINA UNIV OF TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, at present, most of the prodrugs that can realize self-monitoring use fluorescent molecules that do not have therapeutic effects combined with traditional chemotherapy drugs. Observation of prodrug activation at the animal level

Method used

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  • Dimer prodrug and preparation method and application thereof
  • Dimer prodrug and preparation method and application thereof
  • Dimer prodrug and preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment

[0059]A dimer prodrug, its preparation method comprises the following steps (synthetic route such as figure 1 shown):

[0060] 1) Disperse 1.44g (9.0mmol) of 2,3,3-trimethylindole and 7.02g (45.0mmol) of iodoethane in 30mL of acetonitrile, heat to reflux for 24h, then remove the solvent under reduced pressure, and use The crude product obtained by washing with n-hexane was obtained 3 times to obtain (white solid);

[0061] 2) Under a nitrogen atmosphere, mix 3mL (40.95mmol) of dimethylformamide and 15mL of dichloromethane in an ice bath, and then add 20mL of a dichloromethane solution of phosphorus oxychloride (containing phosphorus oxychloride 2.63mL (17.25mmol)) was added dropwise, and 0.74g (7.5mmol) of cyclohexanone was added, heated and stirred to reflux for 3h, then the reaction mixture was poured into ice and left to stand for 12h, filtered to obtain (pale yellow solid);

[0062] 3) 1.89g (6.0mmol) of 0.51g (3.0mmol) and 0.5 g (6.0 mmol) of sodium acetate were...

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Abstract

The present invention discloses a dimer prodrug and a preparation method and an application thereof. A structural formula of the dimer prodrug is shown as follows. The dimer prodrug has a dual fluorescence effect, quenches fluorescences of CyNH2 and DOX through ICT and FRET effects, well monitors an activation process of a drug, also reduces toxicity, also utilizes a synergistic effect of the CyNH2 and DOX, and can also enhance a treatment effect on tumors.

Description

technical field [0001] The invention relates to a dimer prodrug and its preparation method and application, belonging to the technical field of prodrug carriers. Background technique [0002] Tumor treatment mainly includes surgical treatment, chemotherapy, photodynamic therapy, radiotherapy, immunotherapy and other methods, among which chemotherapy is the most important clinical treatment method. However, since the toxicity of chemotherapy drugs is often non-selective, while killing tumor cells, it will also cause great damage to normal tissues, so traditional chemotherapy often brings serious side effects. Therefore, researchers are paying more and more attention to the study of prodrugs. [0003] Prodrugs, also known as prodrugs, drug precursors, prodrugs, etc., refer to drugs that are inactive or less active in vitro after chemical structure modification, and release active drugs through enzymatic or non-enzymatic conversion in vivo. Compounds that exert medicinal prop...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/252C07H1/00A61K31/7056A61P35/00C09K11/06A61K49/00
CPCA61K49/0021A61P35/00C07H1/00C07H15/252C09K11/06C09K2211/1029C09K2211/1088
Inventor 袁友永姜茂麟王可伟肖炫郑锐
Owner SOUTH CHINA UNIV OF TECH
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