Quinazoline sugar derivative and preparation method and application thereof

Abstract

The invention provides a quinazoline sugar derivative and a preparation method and an application thereof, which are capable of solving the problems of low selection inhibitory activity and water solubility of tyrosine kinase inhibitor in the prior art. The glycosylation method of the quinazoline sugar derivative to quinazoline ring in the invention has easily-obtained raw materials, simple synthesis method, simple and convenient purification mode, better bioactivity, especially obvious inhibitory activity on EGFR, and remarkable anti-tumor effect so that the compound has wide prospect in medicines to prevent or cure tumors. The quinazoline sugar derivative has a structure formula as shown in the specification.

Description

Technical field The invention belongs to the fields of medicinal chemistry and drug synthesis, and relates to a quinazoline sugar derivative, a preparation method thereof, and application of the derivative in the preparation of antineoplastic drugs. Background technique Epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase that can mediate multiple signal transduction pathways, transmit extracellular signals into the cell, and promote the proliferation of normal cells and tumor cells , Differentiation and apoptosis both play important regulatory roles. In tumor tissues, epidermal growth factor receptors can also regulate tumor cell proliferation, survival, tumor tissue angiogenesis, tumor tissue invasion and metastasis, and there is overexpression in tumor cells, which is usually considered to be a poor prognosis of cancer Important sign. The epidermal growth factor receptor family is composed of EGFR (Erb-B1), Erb-B2 (HER-2 / neu), Erb-B3 and Erb-B4. All the ab...

AI Technical Summary

Problems solved by technology

The invention provides a quinazoline sugar derivative and its preparation method and application, which can solve the problem of relatively low selective inhibitory activity for inhibiting tyrosine kinases existing in the prior art, and the quinazoline prepared by the invention The water-solubility of sugar-like derivatives is also relatively good, and the selective inhibitory activity of tyrosine kinase is relatively high, which can be applied to the preparation of drugs for preventing or treating tumors

Images