Polo like kinase1 (PLK1) inhibitor and use thereof

Abstract

The invention relates to the field of pharmaceutical chemistry, in particular to medical use of 34 compounds and medicinal composition containing the compounds, particularly use as Polo like kinase 1 inhibitor. Diseases associated with the Polo like kinase 1 inhibitor include melanoma, liver cancer, kidney cancer, acute leukemia, non-small-cell lung cancer, prostatic cancer, cancerous goiter, skin cancer, colorectal cancer, pancreatic cancer, ovarian cancer, breast cancer, myelodysplastic syndromes, esophageal cancer, gastrointestinal tract cancers or mesothelioma.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to 34 compounds, pharmaceutical compositions containing these compounds and their medical application, especially the application as Polo-like kinase 1 (PLK1) inhibitor. Background technique [0002] In recent years, tumors have surpassed cardiovascular diseases and become the world's leading cause of death. The research on anti-tumor drugs has important academic and practical significance. [0003] Studies have found that almost all tumors are related to uncontrolled cell growth, blocked differentiation, and abnormal apoptosis caused by the disorder of cell cycle regulation mechanism. The frequency of tumor cell division is faster than that of normal cells, and various proteins that regulate microtubule polymerization, centrosome duplication, spindle formation, and cytokinesis are often overexpressed and their activities are enhanced. An important class of traditional anti-tumor...

AI Technical Summary

Problems solved by technology

But in general, there are not many PLK1 inhibitors and their structural types at present, and many reported PLK1 inhibitors are non-specific inhibitors, such as Wortmannin, Scytonemin, Staurosporine, morin, ON-01910 and HMN-214, only BI2536, GSK-461364 and LFM-A13 are selective inhibitors of PLK1

Images