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Development of Phyllanthusmin Derivatives as Anticancer Agents: Pharmacological Optimization and Mechanistic Insight

Huntsman, Andrew C
http://rave.ohiolink.edu/etdc/view?acc_num=osu156338449662965

Abstract Details

2019, Doctor of Philosophy, Ohio State University, Pharmacy.
Natural products were once the only source of medicine and, since the dawn of modern drug discovery, have continued to serve as inspiration for the development of novel pharmaceuticals. The use of purified plant constituents greatly advanced the treatment of cancer towards the end of the 20th century. However, there remain many shortcomings with current treatment options with regards to toxicity, resistance, and overall effectiveness. The phyllanthusmin class of natural products, initially identified in 2006 to consist primarily of arylnaphthalene lignan arabinosyl glycosides, possess potent antiproliferative activity as well as a versatile pharmacophore whose exploration has recently been well studied, but not yet exploited into a known drug. The primary work described herein involves utilizing the phyllanthusmin scaffold to identify a novel anticancer lead compound, its mechanism of action, and develop novel synthetic routes in order to further streamline drug property optimization.
James Fuchs, PhD (Advisor)
Liva Rakotondraibe, PhD (Committee Member)
Mark Mitton-Fry, PhD (Committee Member)
578 p.
Organic Chemistry; Pharmacy Sciences
phyllanthusmin; arylnaphthalene lignan lactone; diphyllin glycoside; anticancer natural product; carbasugar; autophagy; karyopherin; importin; exportin; small-molecule drug development; structure-activity relationships; organic synthesis

Recommended Citations

Citations

  • Huntsman, A. C. (2019). Development of Phyllanthusmin Derivatives as Anticancer Agents: Pharmacological Optimization and Mechanistic Insight [Doctoral dissertation, Ohio State University]. OhioLINK Electronic Theses and Dissertations Center. http://rave.ohiolink.edu/etdc/view?acc_num=osu156338449662965

    APA Style (7th edition)

  • Huntsman, Andrew. Development of Phyllanthusmin Derivatives as Anticancer Agents: Pharmacological Optimization and Mechanistic Insight. 2019. Ohio State University, Doctoral dissertation. OhioLINK Electronic Theses and Dissertations Center, http://rave.ohiolink.edu/etdc/view?acc_num=osu156338449662965.

    MLA Style (8th edition)

  • Huntsman, Andrew. "Development of Phyllanthusmin Derivatives as Anticancer Agents: Pharmacological Optimization and Mechanistic Insight." Doctoral dissertation, Ohio State University, 2019. http://rave.ohiolink.edu/etdc/view?acc_num=osu156338449662965

    Chicago Manual of Style (17th edition)

osu156338449662965
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© 2019, all rights reserved.
This open access ETD is published by The Ohio State University and OhioLINK.