The DOI matches its Crossref record; 6 of the 6 references it cites were found in a registry or an index.
Trisubstituted Acridine Derivatives as Potent and Selective Telomerase Inhibitors
Open accessAbstract
The synthesis and evaluation for telomerase-inhibitory and quadruplex DNA binding properties of three related series of rationally designed trisubstituted acridine derivatives are described. These are substituted on the acridine ring at the 2,6,9; 2,7,9; and 3,6,9 positions. The ability of several of the most potent compounds to interact with and stabilize an intramolecular G-quadruplex DNA was evaluated by surface plasmon resonance methods, and affinities were found to correlate with potency in a telomerase assay. The interactions of a number of compounds with a parallel quadruplex DNA structure were simulated by molecular modeling methods. The calculated interaction energies were compared with telomerase activity and showed generally consistent correlations between quadruplex affinity and telomerase inhibition. These data support a model for the action of these compounds that involves the stabilization of intermediate quadruplex structures that inhibit the elongation of telomeric DNA by telomerase in tumor cells.
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Citations
Cites
Telomeres shorten during ageing of human fibroblasts
Harley, C. B., Futcher, A. B., & Greider, C. W. (1990) · Nature · doi:10.1038/345458a0 · Cited by 5,750
Bryan, T. M., Englezou, A., Dalla-Pozza, L., Dunham, M. A., & Reddel, R. R. (1997) · Nature Medicine · doi:10.1038/nm1197-1271 · Cited by 1,292
Hemann, M. T., Strong, M. A., Hao, L.-Y., & Greider, C. W. (2001) · Cell · doi:10.1016/s0092-8674(01)00504-9 · Cited by 1,219
Telomere maintenance by recombination in human cells
Dunham, M. A., Neumann, A. A., Fasching, C. L., & Reddel, R. R. (2000) · Nature Genetics · doi:10.1038/82586 · Cited by 879
Telomerase activity in human ovarian carcinoma.
Counter, C. M., Hirte, H. W., Bacchetti, S., & Harley, C. B. (1994) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.91.8.2900 · Cited by 677
Herbert, B.-S., Pitts, A. E., Baker, S. I., Hamilton, S. E., Wright, W. E., Shay, J. W., & Corey, D. R. (1999) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.96.25.14276 · Cited by 539
Cited by
Burger, A. M., Dai, F., Schultes, C. M., Reszka, A. P., Moore, M. J., Double, J. A., & Neidle, S. (2005) · Cancer Research · doi:10.1158/0008-5472.can-04-2910 · Cited by 587
Self-citationTargeting telomeres and telomerase
De Cian, A., Lacroix, L., Douarre, C., Temime-Smaali, N., Trentesaux, C., Riou, J.-F., & Mergny, J.-L. (2008) · Biochimie · doi:10.1016/j.biochi.2007.07.011 · Cited by 572
Dexheimer, T. S., Sun, D., & Hurley, L. H. (2006) · Journal of the American Chemical Society · doi:10.1021/ja0563861 · Cited by 383
Fluorescence-based melting assays for studying quadruplex ligands
DECIAN, A., GUITTAT, L., KAISER, M., SACCA, B., AMRANE, S., BOURDONCLE, A., ALBERTI, P., TEULADEFICHOU, M., LACROIX, L., & MERGNY, J. (2007) · Methods · doi:10.1016/j.ymeth.2006.10.004 · Cited by 381
Structural Basis of DNA Quadruplex Recognition by an Acridine Drug
Campbell, N. H., Parkinson, G. N., Reszka, A. P., & Neidle, S. (2008) · Journal of the American Chemical Society · doi:10.1021/ja8016973 · Cited by 326
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Metadata
- Authors
- Harrison, R. J., Cuesta, J., Chessari, G., Read, M. A., Basra, S. K., Reszka, A. P., Morrell, J., Gowan, S. M., Incles, C. M., Tanious, F. A., Wilson, W. D., Kelland, L. R., & Neidle, S.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2003-09-06
- Volume
- 46
- Issue
- 21
- Pages
- 4463-4476
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1987006829
- Cited by
- 186
- References
- 6
- FWCI
- 2.68
- Type
- journal article
- Language
- en
- Open access
- green
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