Honors Theses
Date of Award
2008
Document Type
Undergraduate Thesis
Department
Chemistry and Biochemistry
First Advisor
Mark Hamann
Relational Format
Dissertation/Thesis
Abstract
Kahalalide F (KF, 1) is the largest and most biologically active cyclic peptide of the naturally occurring kahalalide family of depsipeptides. Previous evaluations of the compound have shown significant in vitro and in vivo activity against various forms of cancer. KF has been investigated in phase I clinical trials and is being evaluated in phase II clinical studies. The objective of this experiment was to prepare analogues of KF through semisynthetic modification of the parent compound to optimize activity against a slate of pathogens, as well as cancerous cells. Data revealed that KF and analogues were not active against malaria, leishmania, or bacteria. However, the series was active against various strains of fungi, including Fusarium, a genus known for causing opportunistic infections in plants, as well as humans. KF and analogues were also evaluated for in vitro activity against 60 human cancer cell lines. Analogue 5 exhibited greater activity than 1 against several cell lines, including leukemia, colon, ovarian, renal, and prostate cell lines. Through the evaluations of antiprotozoal, antibacterial, and antifungal activity, as well as the activity against a slate of human cancer cell lines, it was revealed that semisynthetic modification of the parent compound has an affect on activity. Further studies involving semisynthetic modification of KF could lead to vast improvements in current drug therapies.
Recommended Citation
Woodruff, Kully Lynn, "Optimization Studies of the Important Drug Lead Kahalalide F which Acts on a Novel Cancer Target RPS25" (2008). Honors Theses. 2279.
https://egrove.olemiss.edu/hon_thesis/2279
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