SENP2 small molecule inhibitor and applications thereof

Abstract

The invention discloses an SENP2 small molecule inhibitor and applications thereof, and provides the SPNP2 small molecule inhibitor, which contains effective components namely derivatives represented by the formula (I) or pharmaceutically-acceptable salts of the derivatives; wherein the R1 and R2 in the A ring can be chlorine mono-substituted by R1 or chlorine disubstituted by R1 and R2; the Y and Z in the B ring represent a nitrogen atom or a carbon atom; the R3 to R7 in the C ring represent H, halogen, a hydroxyl group, a nitro group, an amino group, a sulfonamide group, a mercapto group, a methoxyl group, an ethoxyl group, a benzyloxy group, a methyl group, and a cyano group; T, U, V, W, and X represent a nitrogen atom or a carbon atom; and C ring can be a phenyl ring, a pyridine ring, a furan ring, a thiophene ring, a pyrrole ring, cinnamic acid, or derivatives of cinnamic acid. The high-efficient SENP2 small molecule inhibitor with a low toxicity can prominently inhibit the activity of SENP2, can be used to prepare drugs for treating breast cancer, and thus has a very important meaning in development of antitumor drugs.

Description

technical field [0001] The invention relates to the field of medicinal chemotherapy, in particular to a SENP2 small molecule inhibitor and its application as a drug compound for preventing or treating breast cancer. Background technique [0002] Breast cancer is one of the malignant tumors of women. According to statistics, the incidence rate accounts for 7-10% of various malignant tumors in the whole body. Its incidence is often related to heredity, and the incidence rate is higher in women between the ages of 40 and 60 and before and after menopause. Only about 1-2% of breast cancer patients are men. Malignant tumors that usually occur in breast epithelial tissue are one of the most common malignant tumors that seriously affect women's physical and mental health and even threaten their lives. Male breast cancer is rare. [0003] There are a variety of protein covalent modification methods in cells, such as phosphorylation, acetylation, ubiquitination, methylation, etc., ...

AI Technical Summary

Problems solved by technology

Due to the necessity of SENP2 in the process of cell and organism development, the use of biotechnology in the study of its mechanism is limited to a certain extent, which hinders the in-depth exploration of the research on the developmental signaling pathways mediated by it and related diseases

Using drug design methods, we found a series of chemical small molecules that can effectively inhibit the activity of SENP2 through screening and in vitro activity detection (currently there is no SENP2 regulatory small molecule published internationally)

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