CDK6/DYRK2 double-target inhibitor as well as preparation method and application thereof
Patent Information
- Authority / Receiving Office
- CN · China
- Current Assignee / Owner
- JIANGSU TASLY DIYI PHARMA CO LTD
- Publication Date
- 2021-02-23
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Abstract
Description
technical field
[0001] The invention relates to the field of medicinal chemistry, in particular to a CDK6 / DYRK2 dual-target inhibitor and its preparation method and application. Background technique
[0002] Cyclin-dependent kinase 6 (CDK6 ) is a serine / tyrosine kinase that regulates the transition from the G1 phase to the S phase of the cell cycle. In the early stage of the G1 phase of the cell cycle, cyclin D binds to CDK6 and activates CDK6, and the formed cyclin D-CDK6 complex can promote the phosphorylation of retinoblastoma protein (Rb). Phosphorylation of Rb leads to the release of the transcription factor E2F, which accelerates the progression of the cell cycle from G1 phase to S phase. The up-regulation of the proto-oncogene CDK6 will lead to the acceleration of the process of cell cycle from G1 phase to S phase, resulting in the acceleration of cell cycle and cell proliferation. Uncontrolled cell proliferation is the main feature of cancer, therefore, the inhibit...