Highly Stable Phenanthridinium Frameworks as a New Class of Tunable DNA Binding Agents with Cytotoxic Properties

A new class of cytotoxic heteroaromatic cations is presented, based on the dihydro-imidazo-phenanthridinium framework (DIP), that have affinity for DNA and cytotoxicity toward cancerous cells. The DIP framework is particularly tunable due to the flexible synthetic methodology. Furthermore, the centr...

Full description

Saved in:
Bibliographic Details
Published in:Journal of medicinal chemistry 2005-07, Vol.48 (14), p.4504-4506
Main Authors: Parenty, Alexis D. C, Smith, Louise V, Guthrie, Kevin M, Long, De-Liang, Plumb, Jane, Brown, Robert, Cronin, Leroy
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
Cell Line, Tumor
Crystallography, X-Ray
DNA - metabolism
Drug Screening Assays, Antitumor
General aspects
Humans
Imidazoles - chemical synthesis
Imidazoles - chemistry
Imidazoles - pharmacology
Intercalating Agents - chemical synthesis
Intercalating Agents - chemistry
Intercalating Agents - pharmacology
Medical sciences
Pharmacology. Drug treatments
Phenanthridines - chemical synthesis
Phenanthridines - chemistry
Phenanthridines - pharmacology
Structure-Activity Relationship
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:A new class of cytotoxic heteroaromatic cations is presented, based on the dihydro-imidazo-phenanthridinium framework (DIP), that have affinity for DNA and cytotoxicity toward cancerous cells. The DIP framework is particularly tunable due to the flexible synthetic methodology. Furthermore, the central moiety has proved to be very stable to hydrolysis and reduction compared to other phenanthridinium-based agents.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm050320z