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5,8-disubstituted-1,6-quinazoline-7-amidocarbonylation compound, preparing method, composite and application thereof

A phthalazine and disubstituted technology, which is applied in drug combination, organic chemistry, pharmaceutical formulation, etc., can solve the problem of blocking the growth of tumor cells

Inactive Publication Date: 2010-03-31
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, if PTK activity can be inhibited, it is possible to block the growth of tumor cells

Method used

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  • 5,8-disubstituted-1,6-quinazoline-7-amidocarbonylation compound, preparing method, composite and application thereof
  • 5,8-disubstituted-1,6-quinazoline-7-amidocarbonylation compound, preparing method, composite and application thereof
  • 5,8-disubstituted-1,6-quinazoline-7-amidocarbonylation compound, preparing method, composite and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0064] Anti-tumor activity test:

[0065] Typical compounds in the present invention and their targets against various tumor cells (MDA-MB-435, Hct116p53- / -, Hct116p53+ / +, Mcf-7, NIH 189, SkBr-3, LnCap, LnHer, HT 29, HEY) The semi-growth inhibitory activity data (IC 50 ) were measured under standard conditions.

[0066] Example: growth inhibition experiments of compounds on human breast cancer cells MDA-MB-435 and SKBr-3.

[0067] (1) Production methods and sources of main reagents

[0068] RPMII640 was purchased from Gibco; sulforhodamine B was purchased from Sigma; trichloroacetic acid (TCA), acetic acid (HAC) and Tris base unbuffer were all analytically pure.

[0069] (2) Experimental procedure (sulfonylrhodamine B (SRB) protein staining method)

[0070] According to the growth rate of the cells, human breast cancer cells MDA-MB-435 and SKBr-3 in the logarithmic growth phase were inoculated in 96-well culture plates at 90 μl / well, grown adherently for 24 hours, and then...

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Abstract

The invention discloses a 5,8-disubstituted-1,6-quinazoline-7-amidocarbonylation compound, a preparing method, an application and a drug composite containing the compound thereof. More specifically, the invention discloses a 5,8-disubstituted-1,6-quinazoline-7-amidocarbonylation compound as shown in the formula I, a preparing method and an application thereof. By the growth inhibition test of various tumour cell lines (human breast cancer cells MDA-MB-435, p53-deleted poorly differentiated colorectal adenocarcinoma cells Hct116p53- / -, p53-enriched poorly differentiated colorectal adenocarcinoma cells Hct116p53+ / +, human breast cancer cells Mcf-7, NIH189, human breast cancer cells SkBr-3, prostatic cancer cells LnCap, LnHer, human colorectal cancer cells HT29 and human ovarian cancer cellsHEY), the compound has favourable inhibition activity for the above tumour cells and can treat diseases caused by tumour cell malignant proliferation. The invention also discloses a drug composite containing the compound.

Description

technical field [0001] The present invention relates to the field of medical technology, in particular to 5,8-disubstituted-1,6-naphthyridine-7-carbonamide compounds, and the present invention also relates to 5,8-disubstituted-1,6-diazepine The preparation method of naphthalene-7-carbonamide compound. Growth inhibition experiments of various tumor cells (MDA-MB-435, Hct116p53- / -, Hct116p53+ / +, Mcf-7, NIH189, SkBr-3, LnCap, LnHer, HT29, HEY) showed that this type of compound has good anti- Tumor activity can be used to treat diseases caused by malignant proliferation of tumor cells. The present invention also relates to pharmaceutical compositions comprising the compounds described above. Background technique [0002] Tumor (Cancer, tumor, neoplasm) is characterized by abnormal proliferation of cells or mutant cells, often forming a mass. Human tumors are clinically divided into two categories, benign and malignant. Benign tumors (Benignneoplasm) are called tumors. Malig...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K31/4375A61P35/00
CPCC07D519/00C07D471/04A61K31/535A61K31/496A61K31/4375A61P35/00
Inventor 龙亚秋曾立凡王勇丁健
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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