Human telomerase inhibition by substituted acridine derivatives

A series of 3,6-disubstituted acridine derivatives have been rationally designed as telomerase inhibitors. They have been designed on the basis that inhibition of telomerase occurs by stabilising G-quadruplex structures formed by the folding of telomeric DNA. The most potent inhibitors have IC 50 va...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters Jg. 9; H. 17; S. 2463 - 2468
Hauptverfasser: Harrison, R. John, Gowan, Sharon M., Kelland, Lloyd R., Neidle, Stephen
Format: Journal Article
Sprache:Englisch
Veröffentlicht: Oxford Elsevier Ltd 06.09.1999
Elsevier
Schlagworte:
Acridines - chemistry
Acridines - pharmacology
Antineoplastic agents
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
Drug Screening Assays, Antitumor
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
General aspects
Humans
Medical sciences
Pharmacology. Drug treatments
Telomerase - antagonists & inhibitors
Tumor Cells, Cultured
Antineoplastic agent
Human
Enzyme
Aminoamide
Nitrogen heterocycle
Transferases
Acridine derivatives
Enzyme inhibitor
Cytotoxicity
Tricyclic compound
In vitro
Ovary
Nucleotidyltransferases
Cell line
Structure activity relation
Tertiary amine
Aromatic compound
Chemical synthesis
DNA-directed DNA polymerase
ISSN:0960-894X, 1464-3405
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Beschreibung
Zusammenfassung:A series of 3,6-disubstituted acridine derivatives have been rationally designed as telomerase inhibitors. They have been designed on the basis that inhibition of telomerase occurs by stabilising G-quadruplex structures formed by the folding of telomeric DNA. The most potent inhibitors have IC 50 values against telomerase of between 1.3 and 8 μM, comparable to their cytotoxicity in ovarian cancer cell lines.
Bibliographie:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00394-7