Abstract: The present invention discloses a 7-carbonylstaurosporine derivative, a preparation method therefor, and use thereof. The present invention further discloses a chemical synthesis method for 18 typical compounds of this type, which has a simple synthetic route, is easy to operate and implement, and has easily purchasable required reagents. The compounds disclosed in the present invention have significant inhibitory activity against a PIM-1 kinase and excellent kinase selectivity, and can be used for development of therapeutic drugs for related diseases or disorders caused by abnormal expression of the PIM-1 kinase.