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...

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Veröffentlicht in:	Journal of medicinal chemistry 2005-07, Vol.48 (14), p.4504-4506
Hauptverfasser:	Parenty, Alexis D. C, Smith, Louise V, Guthrie, Kevin M, Long, De-Liang, Plumb, Jane, Brown, Robert, Cronin, Leroy
Format:	Artikel
Sprache:	eng
Schlagworte:	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
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Zusammenfassung:	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