A kind of belinostat derivative based on formic acid and its preparation method and application

Abstract

The invention provides a belinostat derivative based on formic acid, and a preparation method and applications thereof. According to the belinostat derivative based on formic acid, belinostat with anti-tumor activity is taken as a parent drug, the dissolvability of belinostat is improved via introduction of water-soluble substituent groups via reaction, so that the dissolvability of the belinostat derivative based on formic acid is excellent, and side effects caused by the poor dissolvability of belinostat are avoided. The steps of the preparation method are few; operation is simple; and the preparation method is suitable for large scale production.

Description

technical field

[0001] The invention relates to the field of antineoplastic drugs, in particular to a formic acid-based belistat derivative and its preparation method and application. Background technique

[0002] Belinostat Belongs to the hydroxamic acid class of histone deacetylase inhibitors (HDACi). The overexpression or abnormal regulation of histone deacetylase (HDAC) will lead to excessive deacetylation of histones, which will remodel chromatin into a configuration that inhibits transcription, resulting in a decrease in the expression of corresponding genes, leading to carcinogenesis. Therefore, inhibition of HDACs is considered a promising anticancer drug target. Belinostat can directly act on the abnormal expression of genes, thereby inhibiting and correcting the excessive proliferation and abnormal differentiation of tumor cells. For common drug resistance problems, it can also be used in combination with drugs with other mechanisms of action. Belinostat can ef...

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