Series of quinazoline sugar derivatives used as protein tyrosine kinase inhibitor, preparation method and application thereof

Abstract

The invention provides a quinazoline sugar derivative and a preparation method and application thereof, which can solve the problem of low activity of inhibiting tyrosine kinase in the prior art. The prepared quinazoline sugar derivative has high water solubility and high activity of inhibiting human skin cancer cells A431, and can be used for preparing medicaments for preventing or treating tumors. The quinazoline sugar derivative provided by the invention is a kind of compounds which have novel structures and comprise abundant glycosyl group segments at a 6-bit side chain of a quinazoline parent ring, wherein the raw materials adopted in a method for performing glycosylation on quinazoline rings are readily available; the synthesis method is simple; the purification mode is simple and convenient and quick; and the quinazoline sugar derivative has high water solubility, high biological activity, particularly obvious activity of selectively inhibiting an EGFR, and obvious anti-tumor effect, so the kind of compounds has a wide application prospect in medicaments for preventing or curing tumors. The quinazoline sugar derivative comprises the following structural formula.

Description

technical field The invention relates to a class of tyrosine kinase inhibitors, in particular to a series of sugar derivatives based on quinazoline parent rings, their preparation methods and their application in the preparation of antitumor drugs. Background technique Targeted therapy is a treatment that uses specific genes or gene expression products that can be expressed by tumor cells but rarely or not expressed by normal cells to form relative or absolute targeting to kill tumor cells to the greatest extent while causing little damage to normal cells method. Tyrosine kinases are a class of transmembrane proteins, enzymes that catalyze the transfer of a phosphate group from ATP to a tyrosine residue located on a protein substrate. Plays an important role in normal cell growth. The epidermal growth factor receptor (EGFR) in the tyrosine kinase family has been identified as an essential enzyme in the process of cell growth and reproduction. In most tumors, the epidermal ...

Images