The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Synthesis and Evaluation of Quindoline Derivatives as G-Quadruplex Inducing and Stabilizing Ligands and Potential Inhibitors of Telomerase
Abstract
A new series of quindoline derivatives (4a-j) were designed and synthesized to develop novel and potent telomerase inhibitors. The interaction of the G-quadruplex of human telomere DNA with these newly designed molecules was examined via circular dichroism spectroscopy and electrophoretic mobility shift assay (EMSA). The selectivity between the quindoline derivative (4a) and G-quadruplex or duplex DNA was investigated by competition dialysis. These new compounds as inhibitors of telomerase were also investigated through the utilization of modified telomerase repeat amplification protocol (TRAP) assay. The results revealed that the introduction of electron-donating groups such as substituted amino groups at the C-11 position of quindoline significantly improved the inhibitory effect on telomerase activity ((Tel)IC50 > 138 microM for quindoline, 0.44-12.3 microM for quindoline derivatives 4a-j). The quindoline derivatives not only stabilized the G-quadruplex structure but also induced the G-rich telomeric repeated DNA sequence to fold into quadruplex.
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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
Structure and function of telomeres
Blackburn, E. H. (1991) · Nature · doi:10.1038/350569a0 · Cited by 3,596
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
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
Targeting 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
Dai, J., Carver, M., Hurley, L. H., & Yang, D. (2011) · Journal of the American Chemical Society · doi:10.1021/ja205646q · Cited by 381
Ma, D.-L., Che, C.-M., & Yan, S.-C. (2009) · Journal of the American Chemical Society · doi:10.1021/ja806045x · Cited by 289
Metadata
- Authors
- Zhou, J.-L., Lu, Y.-J., Ou, T.-M., Zhou, J.-M., Huang, Z.-S., Zhu, X.-F., Du, C.-J., Bu, X.-Z., Ma, L., Gu, L.-Q., Li, Y.-M., & Chan, A. S.-C.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2005-10-15
- Volume
- 48
- Issue
- 23
- Pages
- 7315-7321
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1979395573
- Cited by
- 175
- References
- 3
- FWCI
- 2.65
- Type
- journal article
- Language
- en
- Open access
- closed
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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