Synthesis and biological evaluation of polyamine DNA-intercalator conjugates

Keywords

Spermidine conjugates, Acridine intercalator, Anthracene intercalator, DNA intercalation binding assays, Topoisomerase II inhibition assays

Abstract

One of the major shortcomings of current cancer therapies is the non­selective delivery of the antineoplastic drug to both targeted tumor cells and healthy cells. Enhanced targeting of such drugs could diminish their associated toxicity by reducing their uptake by healthy cells. The strategy delineated in this thesis outlines a new vectoring technology which should direct drugs into specific cell types. Four conjugates (1-4) were synthesized which tether a DNA intercalator (e.g., an acridine or anthracene ring system) to a naturally occurring polyamine (spermidine). The ability of these conjugates to bind to DNA in vitro and to disrupt the proper functioning of topoisomerase II, an enzyme involved in DNA replication was evaluated. These preliminary studies may lead to a new class of vectored chemotherapeutics.

Notes

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Graduation Date

1998

Semester

Spring

Advisor

Phanstiel, Otto

Degree

Master of Science (M.S.)

College

College of Arts and Sciences

Department

Chemistry

Format

PDF

Pages

106 pages

Language

English

Length of Campus-only Access

None

Access Status

Masters Thesis (Open Access)

Identifier

DP0028697

Subjects

Arts and Sciences -- Dissertations; Academic; Dissertations; Academic -- Arts and Sciences; Antineoplastic agents--Synthesis; Drug targeting; DNA-drug interactions; DNA topoisomerase II--Inhibitors; Bioconjugates

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