The DOI matches its Crossref record; 10 of the 10 references it cites were found in a registry or an index.
Human Telomerase Inhibition by Regioisomeric Disubstituted Amidoanthracene-9,10-diones
Open accessAbstract
Telomerase is an attractive target for the design of new anticancer drugs. We have previously described a series of 1,4- and 2, 6-difunctionalized amidoanthracene-9,10-diones that inhibit human telomerase via stabilization of telomeric G-quadruplex structures. The present study details the preparation of three further, distinct series of regioisomeric difunctionalized amidoanthracene-9,10-diones substituted at the 1,5-, 1,8-, and 2,7-positions, respectively. Their in vitro cytotoxicity and Taq DNA polymerase and human telomerase inhibition properties are reported and compared with those of their 1,4- and 2,6-isomers. Potent telomerase inhibition (telIC50 values 1.3-17.3 microM) is exhibited within each isomeric series. In addition, biophysical and molecular modeling studies have been conducted to examine binding to the target G-quadruplex structure formed by the folding of telomeric DNA. These studies indicate that the isomeric diamidoanthracene-9,10-diones bind to the human telomeric G-quadruplex structure with a stoichiometry of 1:1. Plausible G-quadruplex-ligand complexes have been identified for each isomeric family, with three distinct modes of intercalative binding being proposed. The exact mode of intercalative binding is dictated by the positional placement of substituent side chains. Furthermore, in contrast to previous studies directed toward triplex DNA, it is evident that stringent control over positional attachment of substituents is not a necessity for effective telomerase inhibition.
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Citations
Cites
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The RNA Component of Human Telomerase
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Telomere Shortening and Tumor Formation by Mouse Cells Lacking Telomerase RNA
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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
Telomere maintenance as a target for anticancer drug discovery
Neidle, S., & Parkinson, G. (2002) · Nature Reviews Drug Discovery · doi:10.1038/nrd793 · Cited by 624
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
Telomerase inhibitors based on quadruplex ligands selected by a fluorescence assay
Mergny, J.-L., Lacroix, L., Teulade-Fichou, M.-P., Hounsou, C., Guittat, L., Hoarau, M., Arimondo, P. B., Vigneron, J.-P., Lehn, J.-M., Riou, J.-F., et al. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.051620698 · Cited by 291
Metadata
- Authors
- Perry, P. J., Reszka, A. P., Wood, A. A., Read, M. A., Gowan, S. M., Dosanjh, H. S., Trent, J. O., Jenkins, T. C., Kelland, L. R., & Neidle, S.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 1998-10-31
- Volume
- 41
- Issue
- 24
- Pages
- 4873-4884
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2060389234
- Cited by
- 165
- References
- 10
- FWCI
- 3.26
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: Human Telomerase Inhibition by Regioisomeric Disubstituted Amidoanthracene-9,10-diones. https://app.cochat.ai/papers/10.1021/jm981067o
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- Perry, P. J., Reszka, A. P., Wood, A. A., Read, M. A., Gowan, S. M., Dosanjh, H. S., Trent, J. O., Jenkins, T. C., Kelland, L. R., & Neidle, S. (1998). Human Telomerase Inhibition by Regioisomeric Disubstituted Amidoanthracene-9,10-diones. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm981067o
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