Submission Date
4-29-2025
Document Type
Paper- Restricted to Campus Access
Department
Chemistry
Adviser
Julianne Yost
Committee Member
Eric Williamsen
Department Chair
Mark Ellison
External Reviewer
Russell Kielawa
Distinguished Honors
This paper has met the requirements for Distinguished Honors.
Project Description
Cancer continues to be a leading cause of death worldwide and occurs when improper gene regulation leads to uncontrolled cell growth. Methyltransferases are a large class of enzymes that regulate gene expression through methylation, and overexpression of methyltransferases has been linked to numerous human diseases, including cancer. Given the important role of methyltransferases in human disease, a selective small molecule inhibitor would be a valuable contribution to the field. In this study, amide coupling reactions were explored to modify a core scaffold at key positions. The standard amide coupling reagents and purification conditions were compared to optimize product yield and purity. A previously developed deprotection procedure was also applied to fifteen compounds in our current library, and the crude desired products were characterized using NMR, HPLC, and LC-MS. Once the final compounds have been fully synthesized, purified, and characterized, all compounds in the library will be evaluated for their potency and selectivity against different methyltransferases. A library of structurally similar yet unique compounds will enable a structure activity relationship (SAR) study to determine the effect of the various groups on enzyme activity.
Recommended Citation
Miller, Alannah E., "Synthesis, Purification, and Characterization of Potential Small Molecule Methyltransferase Inhibitors" (2025). Chemistry Honors Papers. 78.
https://digitalcommons.ursinus.edu/chem_hon/78
