Dipeptide boric acid composed of carboxylic acid and alpha-amino acid as well as ester compound thereof, and preparation method and application of dipeptide boric acid and ester compound thereof

Abstract

The invention belongs to the field of drug synthesis and in particular relates to a series of novel peptide boric acids as well as an ester compound or pharmaceutical salt thereof, and a preparation method and application of the peptide boric acids as well as the ester compound or pharmaceutical salt thereof in pharmacodynamics. A structure of the peptide boric acid and the ester compound or pharmaceutical salt thereof is shown in a formula I (described in the specification). The compound provided by the invention can be used for preparing a proteasome inhibitor and can further be used for treating solid tumours and blood tumours, wherein the solid tumours are selected from non-small cell lung cancer, small cell lung cancer, lung adenocarcinoma, lung squamous carcinoma, pancreatic cancer, breast cancer, prostate cancer, liver cancer, skin cancer, epithelial cell cancer, gastrointestinal stromal tumor, nasopharynx cancer and leukemia; and the blood tumours are selected from multiple myeloma, mantle cell lymphoma and histiocytic lymphoma.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and in particular relates to a series of preparation methods of novel peptide boronic acid and its ester compounds and their application in pharmacodynamics. Background technique [0002] At present, cancer is one of the most important diseases that endanger human health. Although the current treatment of cancer has made great progress in the fields of surgical treatment, chemotherapy, and radiotherapy, it still cannot fundamentally treat cancer. Although the currently marketed anticancer drugs have certain curative effects, they have serious toxic and side effects. Therefore, in-depth exploration and research on how to start from effective tumor targets to study targeted new anticancer drugs has become a top priority for medical workers. [0003] The Ubiquitin-Proteasome Pathway (UPP) is the main pathway for the degradation of intracellular protein systems and is involved in many physiologically ...

AI Technical Summary

Problems solved by technology

The price of Velcade in the Chinese market is about 13,000 yuan per 3.5 mg, and the cost of one cycle of treatment is about 40,000 yuan. Such an expensive cost is a very heavy financial burden for many patients

Moreover, current clinical data show that these drugs also have more side effects, such as fatigue, nausea, diarrhea, and neuropathy.

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