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

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...

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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 activities, due to their strong hydrophilicity, it is difficult to penetrate the lipid bilayer of biological membranes and affect their pharmacological effects (Wang Rutao, Zhou Yuan , Zhang Feng, et al. Protective effect of ethyl ferulate on human vascular endothelial cells injured by hydrogen peroxide[J]. Chinese Clinical Pharmacology and Therapeutics, 2004, 9(7): 763-765. Applications of Compounds

Chinese patent 201010214044.6 reports aromatic acid prodrugs with nitric oxide donors and their preparation methods and applications, but there is no use of aromatic acid derivatives with nitric oxide donors in anti-malignant tumor drugs Applied coverage

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