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Synthetic studies on anti-cancer and...
~
Headrick, Sarah Autumn.
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Synthetic studies on anti-cancer and anti-HIV compounds.
Record Type:
Electronic resources : Monograph/item
Title/Author:
Synthetic studies on anti-cancer and anti-HIV compounds./
Author:
Headrick, Sarah Autumn.
Description:
325 p.
Notes:
Source: Dissertation Abstracts International, Volume: 64-09, Section: B, page: 4355.
Contained By:
Dissertation Abstracts International64-09B.
Subject:
Chemistry, Organic. -
Online resource:
http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=3104387
Synthetic studies on anti-cancer and anti-HIV compounds.
Headrick, Sarah Autumn.
Synthetic studies on anti-cancer and anti-HIV compounds.
- 325 p.
Source: Dissertation Abstracts International, Volume: 64-09, Section: B, page: 4355.
Thesis (Ph.D.)--The University of Tennessee, 2003.
The research discussed in this dissertation focuses on the synthesis and biological evaluation of two families of therapeutic agents.Subjects--Topical Terms:
516206
Chemistry, Organic.
Synthetic studies on anti-cancer and anti-HIV compounds.
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325 p.
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Source: Dissertation Abstracts International, Volume: 64-09, Section: B, page: 4355.
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Adviser: David C. Baker.
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Thesis (Ph.D.)--The University of Tennessee, 2003.
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The research discussed in this dissertation focuses on the synthesis and biological evaluation of two families of therapeutic agents.
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In 1999 a group of scientists at the National Cancer Institute reported that during a screening of their database they had found an active non-nucleoside reverse transcriptase inhibitor. This compound (NSC-108406) was substantially more potent than the other inhibitors identified during their screening with an IC50 of 0.5 +/- 0.3 muM. During a cell-based antiviral screen, it was found to provide an EC50 of 1.5 +/- 1.0 muM. In an effort to increase the potency of the lead, a set of analogs of NSC-108406 was synthesized in our laboratories, providing a compound with an EC 50 of 0.036 muM.
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Hydramycin is a naturally occurring pluramycinone that is a potent antimicrobial and antitumor agent and whose biological activity has created an interest in its synthesis. Our work began with a model study that established a strategy by which the pyranone system and associated functionality could be realized. The route makes use of a novel alkyne and a fluoride-induced ring closure that provided a molecule consisting of a chromenone with the essential moieties analogous to those of hydramycin. The protocol was applied to a compound containing the hydramycin anthraquinone system via a 2-formyl-1-hydroxy anthraquinone that was coupled with an alkyne.
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http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=3104387
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