Pyrido[2,3-b][1,5]benzoxazepin-5(6H)-one derivatives as CDK8 inhibitors

CDK8 is a cyclin-dependent kinase that forms part of the mediator complex, and modulates the transcriptional output from distinct transcription factors involved in oncogenic control. Overexpression of CDK8 has been observed in various cancers, representing a potential target for developing novel CDK...

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Bibliographic Details
Published in:	European journal of medicinal chemistry Vol. 201; p. 112443
Main Authors:	Martínez-González, Sonia, García, Ana Belén, Albarrán, M. Isabel, Cebriá, Antonio, Amezquita-Alves, Adrián, García-Campos, Francisco Javier, Martínez-Gago, Jaime, Martínez-Torrecuadrada, Jorge, Muñoz, I.G., Blanco-Aparicio, Carmen, Pastor, Joaquín
Format:	Journal Article
Language:	English
Published:	France Elsevier Masson SAS 01-09-2020
Subjects:	CDK8 Cell Line, Tumor Cyclin-Dependent Kinase 8 - antagonists & inhibitors Drug Design Humans Molecular Structure Oxazepines - chemical synthesis Oxazepines - pharmacology P-loop flexibility Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - pharmacology Pyridines - chemical synthesis Pyridines - pharmacology pyrido[2,3-b][1,5]benzoxazepin-5(6H)-one scaffold Selectivity Sorafenib - analogs & derivatives Sorafenib - pharmacology Structure-Activity Relationship Type II inhibitors CDK8 Selectivity Type II inhibitors pyrido[2,3-b][1,5]benzoxazepin-5(6H)-one scaffold P-loop flexibility
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