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Conformationally restricted bis(9-aminoacridine)s : a chemical and biological study

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Call No.	QD401 .J39 1988
Author	Jaycox, Gary Delmar.
Title	Conformationally restricted bis(9-aminoacridine)s : a chemical and biological study
Date	1988
Abstract	A series of conformationally restricted bis(9-amino-acridine) derivatives were designed, synthesized, and then evaluated for their chemical and biological behavior. The novel compounds were prepared by treating selected diamines with a stoichiometric excess of 9-chloroacridine in the presence of warm phenol. CPK space filling molecular models predicted that many of these binuclear agents possessed a geometry that would be ideally suited for DNA bis-inter-calation. A number of these compounds were found to be highly active against L1210 murine leukemia in culture, with ID$\sb{50}$ values falling below 10$\sp{-7}$ M. A variety of other derivatives were also prepared and structure-activity relationships determined. These relationships were fully consistent with a bis-intercalative mode of DNA binding. DNA footprinting analyses suggested that binding was not sequence specific. A more detailed examination of the DNA binding process was limited by the poor aqueous solubility of these agents. The conformationally restricted bis(9-amino-acridine)s were further examined by reverse phase thin layer chromatography and were evaluated for their thioytic and hydrolytic stability under physiologically relevant conditions. Several of these agents were found to be effective inhibitors of protein kinase C in whole cell assays. The origins of this effect remain to be elucidated. Finally, lysosomotropic bis(9-aminoacridine)$\cdot$DNA complexes were prepared and their physical and chemical properties explored.
Description	xiv, 171 leaves : ill. 28 cm
Format	application/pdf
Subject	Acridine.
Issuing Body	Dartmouth Dissertations are made available through the Dartmouth Digital Library.
Degree	Thesis (Ph.D.)--Dartmouth College.
Copyright	All rights reserved. No part of this book may be reproduced in any form by any electronic or mechanical means without permission in writing from the author.
DOI	http://dx.doi.org/10.1349/ddlp.1404

Title	Page 1
Full Text	CONFORMATIONALLY RESTRICTED BIS(9-AMINOACRIDINE)S: A CHEMICAL AND BIOLOGICAL STUDY A Thesis Submitted to the Faculty in partial fulfillment of the requirements for the degree of Doctor of Philosophy by Gary D. Jaycox DARTMOUTH COLLEGE Hanover, New Hampshire May 1988

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