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Applications of V027-0576 in preparation of antitumor drugs

An anti-tumor drug and tumor technology, applied in the direction of anti-tumor drugs, drug delivery, drug combination, etc., can solve the problems of poor prognosis of breast cancer and no target found

Active Publication Date: 2021-04-20
THE FIRST AFFILIATED HOSPITAL HENGYANG MEDICAL SCHOOL UNIV OF SOUTH CHINA
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since triple-negative breast cancer does not express estrogen receptor, progesterone receptor, and human epidermal growth factor receptor 2, it is not suitable for most endocrine therapy and targeted therapy for breast cancer with positive expression of HER-2, ER, and PR. Drugs (such as tamoxifen, Herceptin) are not sensitive, and no other particularly effective targets have been found so far, so the prognosis is worse than other types of breast cancer

Method used

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  • Applications of V027-0576 in preparation of antitumor drugs
  • Applications of V027-0576 in preparation of antitumor drugs
  • Applications of V027-0576 in preparation of antitumor drugs

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Embodiment Construction

[0035] Application of compounds and salts thereof in the preparation of antitumor drugs, the general structural formula of the compound is shown in formula I:

[0036]

[0037] In the formula, X is a halogen.

[0038] In some instances, X=Cl.

[0039]In some examples, the salt is an acid addition acid selected from the group consisting of acetic acid, 2,2-dichloroacetic acid, adipic acid, alginic acid, ascorbic acid, L-aspartic acid, benzenesulfonic acid, benzene Formic acid, 4-acetamidobenzoic acid, butyric acid, (+) camphoric acid, camphor-sulfonic acid, (+)-(1S)-camphor-10-sulfonic acid, capric acid, caproic acid, caprylic acid, cinnamic acid, lemon acid, cyclamate, lauryl sulfate, ethane-1,2-disulfonic acid, ethanesulfonic acid, 2-hydroxyethylsulfonic acid, formic acid, fumaric acid, galactobionic acid, gentisic acid, Glucoheptonic acid, D-gluconic acid, glucuronic acid, glutamic acid, α-ketoglutaric acid, glycolic acid, hippuric acid, hydrobromic acid, hydrochloric a...

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Abstract

The invention discloses applications of V027-0576 in preparation of antitumor drugs. Through researches and discovery, the V027-0576 can effectively inhibit the proliferation of MDA-MB-231 cells; the IC50 value of the V027-0576 is 0.95 [mu]m; the inhibition effects of the V027-0576 is superior to the effects of most drugs for clinical treatment of breast cancer, such as cisplatin, gemcitabine, lapatinib, tamoxifen and 5-FU, gefitinib (of which IC50 values respectively are 21.9 [mu]m, > 40 [mu]m, 12.8 [mu]m, 18.9 [mu]m, 9.6 [mu]m and 7.3 [mu]m); and the V027-0576 is superior to a novel multi-target tyrosine kinase inhibitor DCC-2036 and an AXL specific inhibitor R428.

Description

technical field [0001] The present invention relates to novel pharmaceutical uses of compounds. Background technique [0002] Tumors, especially malignant tumors seriously endanger people's life and health. People have developed a variety of anti-tumor drugs, but the existing classic anti-tumor drugs, especially chemotherapy drugs, have serious side effects. [0003] Among many tumors, breast cancer is the tumor with the highest morbidity and mortality in women. The female mammary gland is composed of skin, fibrous tissue, mammary glands and fat. Breast cancer is a malignant tumor that occurs in the mammary gland epithelial tissue. Triple negative breast cancer (TNBC) refers to breast cancer in which the results of immunohistochemical examination of cancer tissue are negative for estrogen receptor (ER), progesterone receptor (PR) and proto-oncogene Her-2. . This type of breast cancer accounts for 10.0% to 20.8% of all breast cancer pathological types. There are about one...

Claims

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Application Information

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IPC IPC(8): A61K31/4427A61K45/06A61K9/00A61P35/00
Inventor 申莹莹何俊祖旭宇尹丽阳牛余珍
Owner THE FIRST AFFILIATED HOSPITAL HENGYANG MEDICAL SCHOOL UNIV OF SOUTH CHINA
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