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Human telomerase inhibition by substituted acridine derivatives
R J Harrison1, S M Gowan, L R Kelland
1CRC Biomolecular Structure Unit, The Institute of Cancer Research, Sutton, Surrey, UK.
Bioorganic & Medicinal Chemistry Letters
|September 25, 1999
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.