The DOI matches its Crossref record; 7 of the 7 references it cites were found in a registry or an index.
2,7-Disubstituted Amidofluorenone Derivatives as Inhibitors of Human Telomerase
Open accessAbstract
Telomerase is a major new target for the rational design of novel anticancer agents. We have previously identified anthraquinone-based molecules capable of inhibiting telomerase by stabilizing G-quadruplex structures formed by the folding of telomeric DNA. In the present study we describe the synthesis and biological evaluation of a series of analogous fluorenone-based compounds with the specific aims of, first, determining if the anthraquinone chromophore is a prerequisite for activity and, second, whether the conventional cytotoxicity inherent to anthraquinone-based molecules may be reduced by rational design. This fluorenone series of compounds exhibits a broad range of telomerase inhibitory activity, with the most potent inhibitors displaying levels of activity (8-12 microM) comparable with other classes of G-quadruplex-interactive agents. Comparisons with analogous anthraquinone-based compounds reveal a general reduction in the level of cellular cytotoxicity. Molecular modeling techniques have been used to compare the interaction of fluorenone- and analogous anthraquinone-based inhibitors with a human G-quadruplex structure and to rationalize their observed biological activities.
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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
Extension of Life-Span by Introduction of Telomerase into Normal Human Cells
Bodnar, A. G., Ouellette, M., Frolkis, M., Holt, S. E., Chiu, C.-P., Morin, G. B., Harley, C. B., Shay, J. W., Lichtsteiner, S., & Wright, W. E. (1998) · Science · doi:10.1126/science.279.5349.349 · Cited by 4,975
Structure and function of telomeres
Blackburn, E. H. (1991) · Nature · doi:10.1038/350569a0 · Cited by 3,596
Telomere Shortening and Tumor Formation by Mouse Cells Lacking Telomerase RNA
Blasco, M. A., Lee, H.-W., Hande, M. P., Samper, E., Lansdorp, P. M., DePinho, R. A., & Greider, C. W. (1997) · Cell · doi:10.1016/s0092-8674(01)80006-4 · Cited by 2,108
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
Strahl, C., & Blackburn, E. H. (1996) · Molecular and Cellular Biology · doi:10.1128/mcb.16.1.53 · Cited by 335
Severe growth defect in mouse cells lacking the telomerase RNA component
Niida, H., Matsumoto, T., Satoh, H., Shiwa, M., Tokutake, Y., Furuichi, Y., & Shinkai, Y. (1998) · Nature Genetics · doi:10.1038/580 · Cited by 156
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
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
Seenisamy, J., Bashyam, S., Gokhale, V., Vankayalapati, H., Sun, D., Siddiqui-Jain, A., Streiner, N., Shin-ya, K., White, E., Wilson, W. D., et al. (2005) · Journal of the American Chemical Society · doi:10.1021/ja0444482 · Cited by 319
Metadata
- Authors
- Perry, P. J., Read, M. A., Davies, R. T., Gowan, S. M., Reszka, A. P., Wood, A. A., Kelland, L. R., & Neidle, S.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 1999-06-17
- Volume
- 42
- Issue
- 14
- Pages
- 2679-2684
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2019724646
- Cited by
- 226
- References
- 7
- FWCI
- 4.24
- Type
- journal article
- Language
- en
- Open access
- green
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