Advances in Structure Modification and Structure-activity Relationships of MAP3K5 Inhibitor Selonsertib
As the first mitogen-activated protein kinase kinase kinase 5(MAP3K5)inhibitor in the clinical stage,indications of selonsertib in clinical trials included non-alcoholic steatohepatitis,pulmonary arterial hypertension and diabetic kidney disease.Due to its novel and unique structure,it has become the main lead compound for structural design and backbone modification of this class of inhibitors.In recent years,a large number of"me-too"candidates had been obtained from selonsertib by the structure modification.This paper introduces the progress of structure modification strategies and structure-activity relationships of selonsertib from two aspects of skeleton fragment modification and cyclization structure modification,aiming to provide a reference for research in this field.
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