Compound C1 used as histone methyltransferase NSD3 activity inhibitor and application thereof

Abstract

A C1 compound as histone methyltransferase NSD3 activity inhibitor and its pharmaceutical use are disclose. C1 has that chemical structure represent by formula I chemical name: 6-Amino-9-(2-(o-Tolyloxy) ethyl)-9H-Purine-8-Thiol; At least one of that compound C1 or its hydrate, pharmaceutically acceptable salt, tautomers, stereoisomer. And precursor compounds are used as an active ingredient in thepreparation of an anti-tumor drug. Experiments show that the compound C1 of the invention can effectively inhibit the NSD3 enzyme activity. And the IC50 value of the enzyme level is 14.63 +- 3. 85 [mu]mol/L. And the compound C1 has good NSD3 enzyme inhibition effect. As an effective inhibitor of an important tumor target NSD3, the compound of the invention is expected to be used as an active ingredient for preparing an antineoplastic drug. And has a pharmaceutical prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a histone methyltransferase NSD3 activity inhibitor and application thereof. Background technique [0002] Histone methylation is one of the most important modification mechanisms of epigenetic modification. The abnormal expression of histone methylation and its regulator histone methyltransferase is closely related to the occurrence of genetic diseases, autoimmune diseases, aging and cancer, especially in the occurrence and development of tumors. Therefore, histone methyltransferases are regarded as potential new targets for anti-tumor therapy. [0003] In recent years, breakthroughs have been made in the development of inhibitors targeting histone methyltransferases. Currently, the histone methyltransferase EZH2 inhibitor EPZ-6438 (Epizyme Company) entered phase I / II clinical trials in 2014 for the treatment of patients with non-Hodgkin's lymphoma, advanced solid...

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Problems solved by technology

However, in the research field of histone lysine methyltransferase inhibitors, most studies mainly focus on histone lysine methyltransferases such as EZH1 and EZH2, DO

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