Approaches toward the synthesis of a potential cancer therapeutic: an acridine-amino acid assembly

Name

• WINTANA H. BEKELEFollow

Publication Date

4-21-2026

Major

Biology (B.S.B.)

Release Option

Open Access

Faculty Mentor

Dr. Karelle Aiken

Abstract

Even though cancer treatment has come a very long way, there are still gaps in effectively treating the disease and preventing complications caused by the side effects. This is due, in part, to the lack of specificity of current therapeutic drugs. To selectively target cancerous cells, this project focused on the L-type amino acid transporter 1 (LAT1), a protein responsible for transporting large, hydrophobic amino acids. LAT1 is highly expressed in cancer cell tissues and has been extensively investigated as a potential carrier for delivering drugs across biological barriers. Acridines are recognized as promising moieties for anti-tumor treatments. They act through various mechanisms, including DNA intercalation, topoisomerase inhibition, oxidative stress induction, and cell cycle disruption. To enhance acridine’s activity and/or improve its targeted delivery with cancer cells, amino acid-acridine conjugates were designed to mimic the substrates of LAT1. The syntheses of the conjugates utilized aromatic and aliphatic side chain linkages and, in one case, explored the use of a 1,2,3-triazole spacer. Overall, biochemical studies probing the anticancer activities of the various designs yielded the most promising results with the directly linked (no triazole spacer) conjugates.

Recommended Citation

BEKELE, WINTANA H., "Approaches toward the synthesis of a potential cancer therapeutic: an acridine-amino acid assembly" (2026). Honors College Theses. 1095.
https://digitalcommons.georgiasouthern.edu/honors-theses/1095