Functionalization and Modification of Naphthaquinone Analogs as HER2 Kinase Inhibitors

<p>HER2 overexpression in breast cancer tumors predicts lower overall survival. Because of the aggressive nature of HER2 tumors and the association with metastatic disease, the HER2 receptor holds great promise as a therapeutic target in metastatic breast cancer. We are developing small molecule inhibitors that bind to the ATP binding site of the tyrosine kinase domain in order to inhibit tyrosine auto-phosphorylation. This process controls biological pathways that mediate the cell growth. In normal cells this process is highly controlled. We are targeting the modification of the side chain of the hydroxy methyl group of 2-Hydroxy methyl-5,8-dimethoxy-1,4-naphthaquinone. These compounds should inhibit the tyrosine kinase cascade of reactions thereby suppressing the overexpression of HER2 shutting down the tumor growth. The synthesis and characterization of a series of substituted naphthaquinone analogs with different increasing chain lengths will be reported.</p>

Name thesis:degree_name

Master of Science

Discipline thesis:degree_discipline

Department of Chemistry

Year

2014

Author dc:creator

• Lella, Divya Jyothi

Contributors dc:contributor

• Cheryl Stevens (Director), Bangbo Yan, Chad A. Snyder

• Organic Chemistry
• Oncogenes
• Cancer
• Breast Cancer
• Leukemia
• Protein-Tyrosine Kinase
• Cells
• Chemical Actions and Uses
• Chemistry
• Medicinal-Pharmaceutical Chemistry

Repository record dc:identifier

https://digitalcommons.wku.edu/theses/1325

OAI identifier oai:identifier

oai:digitalcommons.wku.edu:theses-2328