Nitrogen-containing heterocyclic compound with kinase inhibitory activity, preparation method and use

Abstract

The invention discloses a nitrogen-containing heterocyclic compound having a kinase inhibiting activity, a preparation method and an application. The nitrogen-containing heterocyclic compound is excellent in CDK kinase inhibiting activity and has inhibition effect on proliferation of a series of tumor cells. In addition, the compound, compared with a contrast compound LEE011, not only has a high activity, but also overcomes some defects of the LEE011 well and has an excellent druggability.

Description

technical field [0001] The invention belongs to the field of medicine, in particular, the invention relates to the preparation and application of a nitrogen-containing heterocyclic compound. Background technique [0002] Cyclin-dependent kinases (CDKs) are a class of serine / threonine kinases that dominate the initiation, progression and termination of the cell cycle. The CDK family is an important signal transduction molecule in cells. The CDK-cyclin complex formed by it and cyclin is involved in the growth, proliferation, dormancy and apoptosis of cells, and is closely related to the occurrence and development of tumors. . [0003] The development of drugs targeting CDK kinases for tumor therapy has attracted extensive attention from major pharmaceutical companies and research institutions. Poor absorption in the body and other conditions limit the clinical application. In recent years, based on the discovery of selective inhibitors of various subtypes of CDK kinases, es...

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Problems solved by technology

[0004] CDK4 / 6 are overactive in many cancers, leading to uncontrolled cell proliferation

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