Application of aromatic acid derivative with nitric oxide donor in preparation of medicines for treating malignant cancers

A technology of anti-tumor drugs and compounds, applied in the field of drugs, can solve the problems of large adverse reactions of patients, strong hydrophilicity of molecules, and influence on drug efficacy, etc., to achieve good inhibition of tumor cell growth, promotion of tumor cell apoptosis, strong Effects of Anti-Multiple Tumor Activity

Active Publication Date: 2012-11-21
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Clinically, the current drugs for treating tumors are effective in anti-tumor effect, and the drugs are highly toxic. While killing tumor cells, they also non-selectively kill white blood cells, lymphocytes and other human immune cells. Low concurrent infection, large adverse reactions in patients, long course of treatment, high cost, and great limitations in clinical use
[0003] Aromatic acid compounds, such as ferulic acid, caffeic acid, cinnamic acid, isoferulic acid and coumaric acid, have been reported to have good antithrombotic activity. It is often used in cardiovascular diseases. Although aromatic acid compounds have various pharmacological a

Method used

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  • Application of aromatic acid derivative with nitric oxide donor in preparation of medicines for treating malignant cancers
  • Application of aromatic acid derivative with nitric oxide donor in preparation of medicines for treating malignant cancers
  • Application of aromatic acid derivative with nitric oxide donor in preparation of medicines for treating malignant cancers

Examples

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Embodiment 2

[0034] Example 2 CCK-8 cell proliferation assay was used to determine the effects of compounds 14, 15 and 16 on the proliferation of human cancer cells in vitro

[0035] 1. The CCK-8 cell proliferation assay was used to determine the compound ( E )-3-(4-Hydroxy-3-methoxyphenyl)acrylic acid-4-[4-benzenesulfonyl-1,2,5-oxadiazole-5-oxo-3-oxyl]-2- Butyl ester, namely compound 14; ( E )-3-(4-Hydroxy-3-methoxyphenyl)acrylic acid-4-[4-benzenesulfonyl-1,2,5-oxadiazole-5-oxo-3-oxyl]-1- Butyl ester, namely compound 15; ( E )-3-(4-Hydroxy-3-methoxyphenyl)acrylic acid-2-{2-[4-benzenesulfonyl-1,2,5-oxadiazole-5-oxo-3-oxyl] -Ethoxy}ethyl ester, that is, compound 16 has the effect on human gastric cancer cell MGC-803, human colon cancer cell SW620, human liver cancer cell SMMC-7721, human renal cancer cell Ketr-3, human breast cancer cell MCF-7, human leukemia Effects on the proliferation of HL-60 cells in vitro.

[0036] 2. Test drugs: Compounds 14, 15, and 16 were diluted to 100uM, 50...

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Abstract

The invention discloses a new application of aromatic acid derivative with nitric oxide donor in preparation of medicines for treating malignant cancers. According to the invention, ferulic acid or caffeic acid derivatives with nitric oxide with strong antitumor activities are screened by a plurality of experiments. The experimental results show that the aromatic acid derivative has good effects of inhibiting the growth of tumor cells and promoting tumor cell apoptosis, and also has strong killing function for various malignant cells, and the application range is wider. Especially, three compounds show very strong activity for resisting various tumors, thereby being expected to be developed to new antitumor drugs; and the three compounds are respectively (E)-3-(4-hydroxy-3-methoxyphenyl) propenoic acid-4-[4-benzenesulfonyl-1,2,5-oxadiazole-5-oxy-3-oxy]-2-butyl ester, (E)-3-(4-hydroxy-3-methoxyphenyl) propenoic acid-4-[4-benzenesulfonyl-1,2,5-oxadiazole-5-oxy-3-oxy]-1-butyl ester, and (E)-3-(4-hydroxy-3-methoxyphenyl) propenoic acid-2-{2-[4-benzenesulfonyl-1,2,5-oxadiazole-5-oxy-3-oxy]-ethyoxyl}ethyl ester.

Description

technical field [0001] The invention relates to a medicine, in particular to the application of aromatic acid derivatives with nitric oxide donors in the preparation of medicines for treating malignant tumor diseases. Background technique [0002] Tumor has become the number one killer threatening human survival in the 21st century, with an average of 6.7 million people dying from various tumor diseases every year. China is one of the countries with a high incidence of cancer in the world. There are 2.2 million new cancer patients each year, accounting for 20% of the global total. There are 4.5 million cancer patients, and the number is growing rapidly every year. Clinically, the current drugs for treating tumors are effective in anti-tumor effect, and the drugs are highly toxic. While killing tumor cells, they also non-selectively kill white blood cells, lymphocytes and other human immune cells. It has low incidence of concurrent infection, large adverse reactions for pati...

Claims

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Application Information

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IPC IPC(8): A61K31/216A61K31/4245A61P35/00A61P35/02
Inventor 唐于平李念光段金廒
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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