Identification of Quinones as Novel PIM1 Kinase Inhibitors.

Funding Source

National Institute on Minority Health and Health Disparities, Louisiana Biomedical Research Network, U.S. Department of Defense

Grant Number

LBRN-P20GM103424, 2G12MD007595-06, W81XWH-11-1-0105


Department of Chemistry

Document Type


Publication Date



PIM1 is a proto-oncogene encoding the serine/threonine PIM1 kinase. PIM1 kinase plays important roles in regulating aspects of cell cycle progression, apoptosis resistance, and has been implicated in the development of such malignancies as prostate cancer and acute myeloid leukemia among others. Knockout of PIM1 kinase in mice has been shown to be non-lethal without any obvious phenotypic changes, making it an attractive therapeutic target. Our investigation of anthraquinones as kinase inhibitors revealed a series of quinone analogs showing high selectivity for inhibition of the PIM kinases. Molecular modeling studies were used to identify key interactions and binding poses of these compounds within the PIM1 binding pocket. Compounds 1, 4, 7 and 9 inhibited the growth of DU-145 prostate cancer cell lines with a potency of 8.21 μM, 4.06 μM, 3.21 μM and 2.02 μM.


DOI: 10.1016/j.bmcl.2016.04.079

PubMed ID: 27173800

Funding text

This research work was funded by the NIH-RCMI ( 2G12MD007595-06 ) from the National Institute on Minority Health and Health Disparities , United States and the startup grant by the Louisiana Cancer Research Consortium . Additional support from the Department of Defense Award , United States ( W81XWH-11-1-0105 ), the Louisiana Biomedical Research Network ( LBRN-P20GM103424 ) is greatfully acknowledged. We thank the NIH-BUILD Grant—TL4MD009607 and the Center for Undergraduate Research at Xavier University of Louisiana for supporting the students who worked on this project. The contents are solely the responsibility of the authors and do not represent the official views of NIH, United States.