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Application of IMB5046 compound in the preparation of antineoplastic drugs

A technology of anti-tumor drugs and compounds, applied in the field of medicine, can solve problems such as neurotoxicity, poor water solubility, and difficult synthesis and purification

Active Publication Date: 2015-11-04
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are other technical deficiencies in commonly used clinical microtubule inhibitors, such as neurotoxicity, poor water solubility, and difficulty in synthesis and purification.

Method used

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  • Application of IMB5046 compound in the preparation of antineoplastic drugs
  • Application of IMB5046 compound in the preparation of antineoplastic drugs
  • Application of IMB5046 compound in the preparation of antineoplastic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0100] Embodiment 1: the preparation of chemical formula I compound

[0101] The implementation steps of this embodiment are as follows:

[0102] 2-(4-morpholinyl)-5-nitrobenzoic acid is dissolved in a mixed solvent composed of toluene and dimethylformamide according to a volume ratio of 1:0.1 to obtain a concentration of 2.0% by weight of 2- (4-morpholino)-5-nitrobenzoic acid solution, which was then stirred at a temperature of 60° C. for 0.8 hours, and then added dropwise with a 50% thionyl chloride toluene solution by weight, wherein 2-( The molar ratio of 4-morpholino)-5-nitrobenzoic acid to thionyl chloride is 1:2, and the reaction is continued for 5 hours at the same temperature. Evaporate to dryness under reduced pressure to obtain a kind of evaporated product W1;

[0103] According to the ratio of evaporated dryness W1 in grams to ether in milliliters is 1:50, let the evaporated dryness W1 be recrystallized in ether at room temperature, and the separated crystals are...

Embodiment 2

[0108] Embodiment 2: the preparation of chemical formula I compound

[0109] The implementation steps of this embodiment are as follows:

[0110] 2-(4-morpholinyl)-5-nitrobenzoic acid was dissolved in a mixed solvent composed of toluene and dimethylformamide at a volume ratio of 1:0.2 to obtain a concentration of 1.0% by weight of 2- (4-Morpholinyl)-5-nitrobenzoic acid solution, which was then stirred at a temperature of 70° C. for 1.2 hours, and then added dropwise with a thionyl chloride toluene solution with a concentration of 58% by weight, wherein 2-( The molar ratio of 4-morpholino)-5-nitrobenzoic acid to thionyl chloride is 1:5, and the reaction is continued for 4 hours at the same temperature, and the obtained reaction solution is carried out under the conditions of temperature 42°C and pressure 0.01MPa Evaporate to dryness under reduced pressure to obtain a kind of evaporated product W1;

[0111] According to the ratio of evaporated dryness W1 in grams to ether in m...

Embodiment 3

[0116] Embodiment 3: the preparation of chemical formula I compound

[0117] The implementation steps of this embodiment are as follows:

[0118] 2-(4-morpholinyl)-5-nitrobenzoic acid was dissolved in a mixed solvent composed of toluene and dimethylformamide at a volume ratio of 1:0.1 to obtain a concentration of 1.6% by weight of 2- (4-morpholino)-5-nitrobenzoic acid solution, which was then stirred at a temperature of 50° C. for 1.0 hour, and then added dropwise with a concentration of 70% by weight in thionyl chloride toluene solution, wherein 2-( The molar ratio of 4-morpholino)-5-nitrobenzoic acid to thionyl chloride is 1:1, and the reaction is continued for 8 hours at the same temperature, and the obtained reaction solution is carried out under the conditions of temperature 44°C and pressure 0.004MPa Evaporate to dryness under reduced pressure to obtain a kind of evaporated product W1;

[0119] According to the ratio of evaporated dryness W1 in grams to ether in millil...

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Abstract

The present invention relates to application of IMB5046 compound in the preparation of antineoplastic drugs. The antineoplastic drug is composed of, by weight, 0.1-99.9% of a compounds shown as a formula I and 0.1-99.9% of pharmaceutically acceptable excipients. The compound shown as formula I can inhibit the polymerization of tubulin and destroy microtubules within cells, has strong cytotoxic activity on tumor cells, especially drug-resistant cells, and can inhibit the growth of xenograft tumor in nude mice. The compound is a tubulin polymerization inhibitor with a novel structure, and has good prospects in developing into antineoplastic drug.

Description

【Technical field】 [0001] The invention belongs to the technical field of medicine. More specifically, the present invention relates to the use of IMB5046 compound in the preparation of antitumor drugs. 【Background technique】 [0002] Microtubules are hollow tubular structures composed of 13 fibrils with a diameter of 22 to 25 nm. Each fibril is linearly arranged by tubulin dimers, which are composed of α and β globulins with similar structures. constitute. Microtubules are an important component of the cytoskeleton and play an important role in maintaining cell shape, cell division, intracellular transport and cell movement. During mitosis, microtubules form the spindle, which ensures proper alignment and precise segregation of chromosomes. Rapid spindle microtubule dynamics make cells during division particularly sensitive to microtubule inhibitors (Nat Rev Drug Discov, 2010, 9:790-803). Microtubule inhibitors alter the polymerization state and dynamics of microtubules,...

Claims

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Application Information

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IPC IPC(8): A61K31/5375A61P35/00C07D295/155
Inventor 郑艳波刘秀均甄永苏弓建华吴淑英许先栋李毅司书毅
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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