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 1999-09, Vol.9 (17), p.2463-2468
Hauptverfasser: Harrison, R. John, Gowan, Sharon M., Kelland, Lloyd R., Neidle, Stephen
Format: Artikel
Sprache:eng
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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.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00394-7