The DOI matches its Crossref record; 12 of the 12 references it cites were found in a registry or an index.
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists
Open accessAbstract
3-(Acylamino)-5-phenyl-2H-1,4-benzodiazepines, antagonists of the peptide hormone cholecystokinin (CCK), are described. Developed by reasoned modification of the known anxiolytic benzodiazepines, these compounds provide highly potent, orally effective ligands selective for peripheral (CCK-A) receptors, with binding affinities approaching or equaling that of the natural ligand CCK-8. The distinction between CCK-A receptors on the one hand and CNS (CCK-B), gastrin, and central benzodiazepine receptors on the other is demonstrated by using the structure-activity profiles of the new compounds. Details of the binding of these agents to CCK-A receptors are examined, and the method of development of these compounds is discussed in terms of its relevance to the general problem of drug discovery.
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Citations
Cites
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Design of potent, orally effective, nonpeptidal antagonists of the peptide hormone cholecystokinin.
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Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists
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Impact of Natural Products on Developing New Anti-Cancer Agents
Cragg, G. M., Grothaus, P. G., & Newman, D. J. (2009) · Chemical Reviews · doi:10.1021/cr900019j · Cited by 1,302
Nicolaou, K. C., Pfefferkorn, J. A., Roecker, A. J., Cao, G.-Q., Barluenga, S., & Mitchell, H. J. (2000) · Journal of the American Chemical Society · doi:10.1021/ja002033k · Cited by 678
Benzodiazepine Peptidomimetics: Potent Inhibitors of Ras Farnesylation In Animal Cells
James, G. L., Goldstein, J. L., Brown, M. S., Rawson, T. E., Somers, T. C., McDowell, R. S., Crowley, C. W., Lucas, B. K., Levinson, A. D., & Marsters, J. C. (1993) · Science · doi:10.1126/science.8316834 · Cited by 630
Diversity-oriented synthesis: Exploring the intersections between chemistry and biology
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Metadata
- Authors
- Evans, B. E., Rittle, K. E., Bock, M. G., DiPardo, R. M., Freidinger, R. M., Whitter, W. L., Lundell, G. F., Veber, D. F., Anderson, P. S., Chang, R. S. L., Lotti, V. J., Cerino, D. J., Chen, T. B., Kling, P. J., Kunkel, K. A., Springer, J. P., & Hirshfield, J.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 1988-12-01
- Volume
- 31
- Issue
- 12
- Pages
- 2235-2246
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2059664977
- Cited by
- 1,456
- References
- 12
- FWCI
- 5.91
- Type
- journal article
- Language
- en
- Open access
- green
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
