The DOI matches its Crossref record; 46 of the 46 references it cites were found in a registry or an index.
In Search of a Novel Anti-HIV Drug: Multidisciplinary Coordination in the Discovery of 4-[[4-[[4-[(1 E)-2-Cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, Rilpivirine)
Abstract
Ideally, an anti-HIV drug should (1) be highly active against wild-type and mutant HIV without allowing breakthrough; (2) have high oral bioavailability and long elimination half-life, allowing once-daily oral treatment at low doses; (3) have minimal adverse effects; and (4) be easy to synthesize and formulate. R278474, a new diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI), appears to meet these criteria and to be suitable for high compliance oral treatment of HIV-1 infection. The discovery of R278474 was the result of a coordinated multidisciplinary effort involving medicinal chemists, virologists, crystallographers, molecular modelers, toxicologists, analytical chemists, pharmacists, and many others.
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Cites
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Cited by
Approved Antiviral Drugs over the Past 50 Years
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Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV.
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Molecular Docking: Principles, Advances, and Its Applications in Drug Discovery
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Metadata
- Authors
- Janssen, P. A. J., Lewi, P. J., Arnold, E., Daeyaert, F., de Jonge, M., Heeres, J., Koymans, L., Vinkers, M., Guillemont, J., Pasquier, E., Kukla, M., Ludovici, D., Andries, K., de Béthune, M.-P., Pauwels, R., Das, K., Clark, Frenkel, Y. V., Hughes, S. H., Medaer, B., De Knaep, F., Bohets, H., De Clerck, F., Lampo, A., Williams, P., & Stoffels, P.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2004-11-06
- Volume
- 48
- Issue
- 6
- Pages
- 1901-1909
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2109893413
- Cited by
- 347
- References
- 46
- FWCI
- 7.84
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: In Search of a Novel Anti-HIV Drug: Multidisciplinary Coordination in the Discovery of 4-[[4-[[4-[(1 E)-2-Cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, Rilpivirine). https://app.cochat.ai/papers/10.1021/jm040840e
- The paper
- Janssen, P. A. J., Lewi, P. J., Arnold, E., Daeyaert, F., de Jonge, M., Heeres, J., Koymans, L., Vinkers, M., Guillemont, J., Pasquier, E., Kukla, M., Ludovici, D., Andries, K., de Béthune, M.-P., Pauwels, R., Das, K., Clark, Frenkel, Y. V., Hughes, S. H., . . . Stoffels, P. (2005). In Search of a Novel Anti-HIV Drug: Multidisciplinary Coordination in the Discovery of 4-[[4-[[4-[(1 E)-2-Cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, Rilpivirine). Journal of Medicinal Chemistry. https://doi.org/10.1021/jm040840e
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
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.
