The DOI matches its Crossref record; 10 of the 10 references it cites were found in a registry or an index.
Trisubstituted Acridines as G-quadruplex Telomere Targeting Agents. Effects of Extensions of the 3,6- and 9-Side Chains on Quadruplex Binding, Telomerase Activity, and Cell Proliferation
Open accessAbstract
The synthesis is reported of a group of 3,6,9-trisubstituted acridine compounds as telomeric quadruplex-stabilizing ligands with systematic variations at the 3-, 6-, and 9-positions. A new microwave-assisted methodology has been developed for trisubstituted acridine synthesis. Structure-activity relationships are reported using surface plasmon resonance and a fluorescence melting assay to examine quadruplex binding, together with a telomerase inhibition assay. These reveal relationships between G-quadruplex stabilization and telomerase inhibition and optimal 3,6- and 9-substituent side-chain lengths for maximal activity. Qualitative molecular modeling using molecular dynamics simulations has been undertaken on four quadruplex-DNA complexes. Long-term exposure of MCF7 cancer cells to a subset of the most active compounds, at doses lower than the IC(50) values, showed that one compound produced a marked decrease in population growth, accompanied by senescence, which is consistent with telomere targeting by this agent.
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Cites
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Senescence Induced by Altered Telomere State, Not Telomere Loss
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Telomerase contributes to tumorigenesis by a telomere length-independent mechanism
Stewart, S. A., Hahn, W. C., O'Connor, B. F., Banner, E. N., Lundberg, A. S., Modha, P., Mizuno, H., Brooks, M. W., Fleming, M., Zimonjic, D. B., et al. (2002) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.182407599 · Cited by 431
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Telomerase Maintains Telomere Structure in Normal Human Cells
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Cited by
A hitchhiker's guide to G-quadruplex ligands
Monchaud, D., & Teulade-Fichou, M.-P. (2008) · Org. Biomol. Chem. · doi:10.1039/b714772b · Cited by 788
Highly Efficient G-Quadruplex Recognition by Bisquinolinium Compounds
De Cian, A., DeLemos, E., Mergny, J.-L., Teulade-Fichou, M.-P., & Monchaud, D. (2007) · Journal of the American Chemical Society · doi:10.1021/ja067352b · Cited by 451
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
Self-citationChemistry in human telomere biology: structure, function and targeting of telomere DNA/RNA
Xu, Y. (2011) · Chemical Society Reviews · doi:10.1039/c0cs00134a · Cited by 323
Metadata
- Authors
- Moore, M. J. B., Schultes, C. M., Cuesta, J., Cuenca, F., Gunaratnam, M., Tanious, F. A., Wilson, W. D., & Neidle, S.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2005-12-21
- Volume
- 49
- Issue
- 2
- Pages
- 582-599
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2055132246
- Cited by
- 206
- References
- 10
- FWCI
- 4.38
- Type
- journal article
- Language
- en
- Open access
- green
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