5-thiazole amide compound and biology application thereof

Abstract

The invention relates to a 5-thiazole amide compound and biology application thereof. The 5-thiazole amide compound has a general formula (I) described in the specification and is used for targeting an AKT/PKB kinase (ATP binding site). Experiments prove that a thiazole amide AKT inhibitor can remarkably inhibit the activity of the AKT kinase in vitro and has strong proliferation inhibition function on various tumor cells with high AKT activity, which indicate that the 5-thiazole amide compound can be used for preparing drugs for resisting tumors.

Description

technical field The invention belongs to the field of chemical medicine, 5-thiazole amide compounds with structural characteristics of formula (I) or pharmaceutically acceptable stereoisomers thereof, or prodrug molecules thereof, pharmaceutical compositions containing such compounds and these compounds or Application of the composition in the preparation of antitumor drugs. Background technique Chemotherapy is one of the important methods to treat tumors, but the anticancer drugs commonly used in clinical practice mainly affect the synthesis of DNA or its precursors, which have poor selectivity, high toxicity, and are prone to drug resistance, thus limiting their use. Over the past 20 years, a large number of new antineoplastic drugs targeting tumor-specific molecular changes have entered the clinic. In this class of drugs, inhibitors targeting tyrosine kinase signal transduction pathways have been most successfully developed, such as Gleevec, Sutent, Iressa, Tarceva, Sora...

AI Technical Summary

Problems solved by technology

However, after the plasmid carrying the AKT active fragment was transfected in MCF-7 breast cancer cells, the sensitivity of MCF-7 cells to radiotherapy decreased significantly.

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