Date of Award
Master of Science (MS)
Dr. Suazette Reid Mooring
Dr. Donald Hamelberg
Dr. Jeremiah Harden
There is a lack of good CXCR4 inhibitors that treat cancer cell metastasis and autoimmune diseases without serious drawbacks. AMD3100 and WZ811 are the CXCR4 antagonists that were the initial structural basis for our new potential therapeutics. Molecular modeling and the principles of drug discovery and design were used to plan the synthesis of the compounds presented here. These compounds were synthesized via reductive amination, and then purified via flash column chromatography or preparatory thin layer chromatography. The small molecules were then characterized via melting point, high resolution MS, 13C, and 1H NMR spectroscopy. The Matrigel invasion assay and binding affinity assay were used to screen the potency of the compounds. Compounds that showed high potency in these assays were then subjected to the carrageenan mouse paw edema test. Two lead compounds have emerged as candidates for further testing (2v, and 2a).
Garcia, Francisco Javier Jr., "Synthesis & Evaluation Of Thiophene Derivatives As CXCR4 Antagonists." Thesis, Georgia State University, 2017.
Available for download on Tuesday, May 01, 2018