Abstract
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 IC50 values against telomerase of between 1.3 and 8 microM, comparable to their cytotoxicity in ovarian cancer cell lines.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acridines / chemistry
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Acridines / pharmacology*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Drug Screening Assays, Antitumor
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Humans
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Telomerase / antagonists & inhibitors*
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Tumor Cells, Cultured
Substances
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Acridines
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Antineoplastic Agents
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Enzyme Inhibitors
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Telomerase