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Oxindole-Based Inhibitors of Cyclin-Dependent Kinase 2 (CDK2): Design, Synthesis, Enzymatic Activities, and X-ray Crystallographic Analysis
Open accessAbstract
Two closely related classes of oxindole-based compounds, 1H-indole-2,3-dione 3-phenylhydrazones and 3-(anilinomethylene)-1,3-dihydro-2H-indol-2-ones, were shown to potently inhibit cyclin-dependent kinase 2 (CDK2). The initial lead compound was prepared as a homologue of the 3-benzylidene-1,3-dihydro-2H-indol-2-one class of kinase inhibitor. Crystallographic analysis of the lead compound bound to CDK2 provided the basis for analogue design. A semiautomated method of ligand docking was used to select compounds for synthesis, and a number of compounds with low nanomolar inhibitory activity versus CDK2 were identified. Enzyme binding determinants for several analogues were evaluated by X-ray crystallography. Compounds in this series inhibited CDK2 with a potency approximately 10-fold greater than that for CDK1. Members of this class of inhibitor cause an arrest of the cell cycle and have shown potential utility in the prevention of chemotherapy-induced alopecia.
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Cited by
Fry, D. W., Harvey, P. J., Keller, P. R., Elliott, W. L., Meade, M., Trachet, E., Albassam, M., Zheng, X., Leopold, W. R., Pryer, N. K., et al. (2004) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.1427.3.11 · Cited by 1,236
Kozakov, D., Grove, L. E., Hall, D. R., Bohnuud, T., Mottarella, S. E., Luo, L., Xia, B., Beglov, D., & Vajda, S. (2015) · Nature Protocols · doi:10.1038/nprot.2015.043 · Cited by 648
Pharmacological inhibitors of cyclin-dependent kinases
Knockaert, M., Greengard, P., & Meijer, L. (2002) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(02)02071-0 · Cited by 537
Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6
Toogood, P. L., Harvey, P. J., Repine, J. T., Sheehan, D. J., VanderWel, S. N., Zhou, H., Keller, P. R., McNamara, D. J., Sherry, D., Zhu, T., et al. (2005) · Journal of Medicinal Chemistry · doi:10.1021/jm049354h · Cited by 513
Untangling tau hyperphosphorylation in drug design for neurodegenerative diseases
Mazanetz, M. P., & Fischer, P. M. (2007) · Nature Reviews Drug Discovery · doi:10.1038/nrd2111 · Cited by 459
Metadata
- Authors
- Bramson, H. N., Corona, J., Davis, S. T., Dickerson, S. H., Edelstein, M., Frye, S. V., Gampe, R. T., Harris, P. A., Hassell, A., Holmes, W. D., Hunter, R. N., Lackey, K. E., Lovejoy, B., Luzzio, M. J., Montana, V., Rocque, W. J., Rusnak, D., Shewchuk, L., Veal, J. M., Walker, D. H., & Kuyper, L. F.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2001-11-02
- Volume
- 44
- Issue
- 25
- Pages
- 4339-4358
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2117263757
- Cited by
- 269
- References
- 0
- FWCI
- 10.16
- Type
- journal article
- Language
- en
- Open access
- green
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- The paper
- Bramson, H. N., Corona, J., Davis, S. T., Dickerson, S. H., Edelstein, M., Frye, S. V., Gampe, R. T., Harris, P. A., Hassell, A., Holmes, W. D., Hunter, R. N., Lackey, K. E., Lovejoy, B., Luzzio, M. J., Montana, V., Rocque, W. J., Rusnak, D., Shewchuk, L., Veal, J. M., . . . Kuyper, L. F. (2001). Oxindole-Based Inhibitors of Cyclin-Dependent Kinase 2 (CDK2): Design, Synthesis, Enzymatic Activities, and X-ray Crystallographic Analysis. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm010117d
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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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