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Compound with tumor responsive drug release function, or pharmaceutical salt of compound, as well as preparation and application of compound

A compound and responsive technology, applied in drug combination, antineoplastic drugs, organic chemistry, etc., can solve the problems of toxic side effects, stimulation, and inability to distinguish tumor cells, etc., and achieve the effect of simple operation, mild conditions, and high reaction yield

Active Publication Date: 2015-03-11
HENAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these cytotoxic agents often cannot distinguish between normal tissue cells and dissimilated tumor cells, and can kill normal tissue cells while producing tumor suppression in application, thus causing systemic toxic side effects, such as hair loss, bone marrow suppression, gastrointestinal tract stimulation, etc.

Method used

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  • Compound with tumor responsive drug release function, or pharmaceutical salt of compound, as well as preparation and application of compound
  • Compound with tumor responsive drug release function, or pharmaceutical salt of compound, as well as preparation and application of compound
  • Compound with tumor responsive drug release function, or pharmaceutical salt of compound, as well as preparation and application of compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Preparation of compounds 7 :

[0036] 1. Compound 1 Synthesis:

[0037] Dissolve 0.32g (3mmol) of mercaptopropionic acid in dry 30mL of dichloromethane, and add 0.57g (3mmol) of EDC?HCl (Chinese name: 1-ethyl-(3-dimethylaminopropyl base) carbodiimide hydrochloride) and 0.34g (3mmol) HOSU (N-hydroxysuccinimide), stirred for 3 hours, added Boc mono-protected propylenediamine 0.574 g (3.3mmol), stirred at room temperature for 12 Hour. After washing three times with water, the crude product was separated by column chromatography (eluent: V 石油醚 :V 丙酮 = 5︰1), to get the compound 1 , yield 23.6%.

[0038] attached Figure 5 for the target compound 1 of 1 HNMR spectrum, the experimental data are as follows:

[0039] 1 H NMR (400 MHz, CDCl 3 ) δ 6.13 (s, 1H), 4.60 (d, J = 91.1 Hz, 1H), 3.38 —3.25 (m, 2H), 3.16 —3.08 (m, 2H), 2.85—2.74 (m, 2H), 2.49 (t, J = 6.7 Hz, 2H), 1.66 —1.58 (m, 1H), 1.56 —1.47 (m, 2H), 1.44 (s, 9H).

[0040] 2. Compounds 2 S...

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Abstract

The invention discloses a compound with a tumor responsive drug release function, or a pharmaceutical salt of the compound, as well as preparation and application of the compound, and belongs to the technical field of drug targeting release. The structural formula of the compound is as shown in the Specifications. The designed and synthesized novel tumor cell-sensitive compound disclosed by the invention can stably exist in the normal physiological environment, can release amsacrine drug when entering into tumor cells and performing a cascade reaction under a high-concentration glutathione environment in the tumor cells, and can be used for prepare a novel targeting antitumor drug. In addition, the preparation method of the compound disclosed by the invention is simple and convenient to operate, moderate in conditions, and high in reaction yield.

Description

technical field [0001] The invention belongs to the technical field of drug targeted release, and in particular relates to a compound with tumor responsive drug release or a pharmaceutically acceptable salt thereof and its preparation and application. Background technique [0002] Tumor is one of the important diseases that seriously threaten human health. In recent years, tumor diseases have many unfavorable factors such as high morbidity, high mortality, easy transfer and large side effects of clinical treatment drugs. Currently, chemotherapy is still the main treatment for most malignant tumors. However, the clinical application of anti-tumor drugs is mainly based on their own cytotoxicity to inhibit the growth of tumor cells, thereby achieving the purpose of inhibiting the development of tumors. However, these cytotoxic agents often cannot distinguish between normal tissue cells and dissimilated tumor cells, and can kill normal tissue cells while producing tumor suppre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D219/10A61P35/00
CPCC07D219/10
Inventor 王建红陈冰高凡齐建国张树峰冬海洋
Owner HENAN UNIVERSITY