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 |
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Hauptverfasser: | , , , |
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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/S0960-894X(99)00394-7 |