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Bridge-linked acridine dimer and preparation method and application thereof

An acridine dimer and bridging technology, which is applied in the field of antineoplastic drugs and medicine, can solve the problems of high mortality, high recurrence rate, and high incidence rate, and achieve the effect of high response rate and simple operation

Inactive Publication Date: 2014-12-24
GUANGXI UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] At present, cancer has become one of the chronic diseases that threaten human health. There are problems such as high morbidity, high mortality, high recurrence rate and difficult treatment.

Method used

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  • Bridge-linked acridine dimer and preparation method and application thereof
  • Bridge-linked acridine dimer and preparation method and application thereof
  • Bridge-linked acridine dimer and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: the preparation of bridging type acridine dimer

[0021] (1) Preparation of 9-bromopropylamine acridine:

[0022] Add 0.85g (4.4mmoL) 9-aminoacridine and 30mL acetone to a 100mL round bottom flask, stir until dissolved, then add 1mL (8.8mmoL) 1,3-dibromopropane, heat and stir in an oil bath to reflux, and react During the process, a yellow solid was gradually formed, and the reaction stopped after 24 hours. After the reaction mixture was cooled to room temperature, it was suction-filtered, and after recrystallization with acetone, yellow needle-like crystals were obtained, namely 9-bromopropylamine acridine, m.p.121-124°C, and the yield was over 70%.

[0023] Its reaction equation is as follows:

[0024]

[0025] (2) Preparation of bridged acridine dimer:

[0026] Into a 50mL round bottom flask, add 0.35g (1mmoL) 9-bromopropylamine acridine and 20mL absolute ethanol in sequence, stir until dissolved, heat, stir and reflux in an oil bath for 10min, sl...

Embodiment 2

[0034] Example 2: In vitro tumor activity experiment

[0035] In vitro cytotoxicity assays were performed using the MTT method. The bridged acridine dimer obtained in Example 1 was reacted with the colon cancer Colo205 cell line for 24 hours, and the results are shown in Table 1.

[0036] Table 1 The half maximal effective concentration (IC) of bridged acridine dimer and colon cancer Colo205 cells 50 )

[0037]

[0038] From the results of Example 2, it can be seen that the bridged acridine dimer of the present invention has strong anti-tumor activity through in vitro anti-tumor experiments. The invention provides a new idea for researching and developing new antitumor drugs.

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Abstract

The invention discloses bridge-linked acridine dimer and a preparation method and application thereof. The bridge-linked acridine dimer has the molecular formula of C29H24N4 and the structural formula which is shown in the description. The bridge-linked acridine dimer is prepared by the following steps: using 9-aminoacridine as an initial reactant, stirring and refluxing the 9-aminoacridine together with 1, 3-dibromopropane in an organic solvent, stirring and refluxing the recrystallized 9-bromopropyl aminoacridine together with the 9-aminoacridine in the organic solvent, and recrystallizing to obtain the bridge-linked acridine dimer. The preparation method for the bridge-linked acridine dimer is simple, and mild in reaction conditions; the yield is relatively high; the bridge-linked acridine dimer has relatively high anti-tumor activity, so that a new research direction is provided for preparation of anti-tumor drugs.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to the field of antitumor drugs, in particular to a bridged acridine dimer and its preparation method and application. Background technique [0002] At present, cancer has become one of the chronic diseases that threaten human health, and there are problems such as high morbidity, high mortality, high recurrence rate and difficult treatment. Acridine is a class of nitrogen-containing organic heterocyclic compounds that has received widespread attention. Because its structure is a macrocyclic conjugated system with a rigid planar structure, it can be used as an intercalator for macromolecules such as DNA. It has anti-tumor, anti-virus, and anti-malarial , antibacterial, bioluminescent probes and treatment of AIDS and other aspects have shown strong physiological activity, and 9-aminoacridine derivatives have shown a wide range of applications and development prospects due to their s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D219/12A61K31/473A61P35/00
CPCC07D219/12
Inventor 霍丽妮梁天坚陈睿李培源苏炜王翔
Owner GUANGXI UNIV OF CHINESE MEDICINE
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