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Substituted benzoic acid nitrogen-containing derivatives and antineoplastic usage thereof

A technology for benzoic acid and medicinal salts, which is applied in the field of substituted benzoic acid nitrogen-containing derivatives and its preparation, and can solve problems such as unsatisfactory, limited universal applicability of drugs, and malignant killing of normal cells

Inactive Publication Date: 2008-04-09
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the specific drugs for the treatment of tumor diseases are not satisfactory, and the malignant killing of normal cells caused by the low selectivity of cytotoxic drugs currently used in anti-tumor clinics limits the general applicability of such drugs

Method used

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  • Substituted benzoic acid nitrogen-containing derivatives and antineoplastic usage thereof
  • Substituted benzoic acid nitrogen-containing derivatives and antineoplastic usage thereof
  • Substituted benzoic acid nitrogen-containing derivatives and antineoplastic usage thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0037] Example 1 : the preparation of compound I-a i.e. 2 '-(3 ", 4 "-dimethoxyaniline)-2'-oxoethyl-benzoic acid ester

[0038]

[0039] This example relates to a general synthesis method of a class of substituted acetylarylamine benzoate derivatives shown in formula (I) with cytotoxic activity. It specifically relates to the preparation of compound 2'-(3",4"-dimethoxyaniline)-2'-oxoethyl-benzoate. Dissolve chloroacetyl 3,4-dimethoxyaniline (78 mg) in 10 ml of DMF, add potassium iodide (90 mg) and stir at 40°C for 20 minutes, then add potassium benzoate (106 mg), and reflux After 4 hours, the DMF was removed by concentration under reduced pressure. The obtained crude product was partitioned and extracted with ethyl acetate-water, and the ethyl acetate layer was washed with water until neutral, washed with saturated sodium chloride solution, and dried overnight with anhydrous sodium sulfate. The obtained filtrate was filtered and concentrated, and purified by column chroma...

Embodiment 2

[0057] Pharmacological Example 2 : Cytotoxic activity of compound I-f on leukemia (HL-60) tumor cells

[0058] Leukemia (HL-60) tumor cells were cultured with RPMI 1640 medium containing 10% fetal bovine serum, 100 U / ml penicillin and 100 U / ml streptomycin. cells in 5×10 per well 3 concentration into a 96-well plate at 37 °C with 5% CO 2 Incubate for 24 hours in a humidified incubator.

[0059] Cell viability was determined by the modified MTT method. After the cells were incubated for 24 hours, the newly prepared dimethyl sulfoxide solution of compound I-f was added to each well in a concentration gradient, so that the final concentrations of the compounds in the wells were 100 μg / ml, 33.3 μg / ml, and 11.1 μg / ml and 3.7 μg / ml. After 72 hours, add 10 microliters of MTT (5 mg / ml) in phosphate buffer, continue to incubate at 37°C for 4 hours, centrifuge for 5 minutes to remove unconverted MTT, and add 200 microliters of dimethyl sulfide to each well. The sulfone was used ...

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Abstract

The invention relates to a nitrogen contained alike derivate and medicine salt or solvolyte which can replace benzoic acid and which has the structure of formula (I) and cytotoxin activeness. The invention also relates to a preparation method for preparation formular(I) compound, the medicine compound and the medical functions. The compound of the invention has relative strong capability for restraining the growth of knub cell of liver cancer (BFL-7404) and leucocythemia (HL-60), and the compound can be used as anti-knub medicine anticipatorily.

Description

field of invention [0001] The present invention relates to the fields of organic chemistry, medicinal chemistry and pharmacology. Specifically, the present invention relates to a class of substituted benzoic acid nitrogen-containing derivatives and a preparation method thereof, and the effects of these compounds on human liver cancer (BEL-7404) and leukemia ( HL-60) cytotoxic activity of tumor cells. Such compounds are found to have certain biological activity of inhibiting the growth of the tumor cells, and can be expected to be used as antitumor drugs. Background of the invention [0002] At present, due to environmental pollution and other problems brought about by industrial development, the quality of human living environment continues to decline, and the incidence and mortality of tumor diseases are also increasing. However, the specific drugs for the treatment of tumor diseases are not satisfactory, and the malignant killing of normal cells caused by the low selecti...

Claims

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Application Information

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IPC IPC(8): C07C235/24A61K31/24A61P35/00
Inventor 黄可新邹宏斌李校堃杨雷香巫秀美赵昱瞿佳
Owner WENZHOU MEDICAL UNIV
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