Human telomerase inhibition by substituted acridine derivatives. |
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Authors: | R J Harrison S M Gowan L R Kelland S Neidle |
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Institution: | CRC Biomolecular Structure Unit, The Institute of Cancer Research, Sutton, Surrey, UK. |
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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. |
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