The DOI matches its Crossref record; 33 of the 33 references it cites were found in a registry or an index.
The role of fluorine in medicinal chemistry: Review Article
Open accessAbstract
The small and highly electronegative fluorine atom can play a remarkable role in medicinal chemistry. Selective installation of fluorine into a therapeutic or diagnostic small molecule candidate can enhance a number of pharmacokinetic and physicochemical properties such as improved metabolic stability and enhanced membrane permeation. Increased binding affinity of fluorinated drug candidates to target protein has also been documented in a number of cases. A further emerging application of the fluorine atom is the use of 18F as a radiolabel tracer atom in the exquisitely sensitive technique of Positron Emission Tomography (PET) imaging. This short review aims to bring together these various aspects of the use of fluorine in medicinal chemistry applications, citing selected examples from across a variety of therapeutic and diagnostic settings. The increasingly routine incorporation of fluorine atom(s) into drug candidates suggests a bright future for fluorine in drug discovery and development. A major challenge moving forward will be how and where to install fluorine in a rational sense to best optimise molecular properties.
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Penning, T. D., Talley, J. J., Bertenshaw, S. R., Carter, J. S., Collins, P. W., Docter, S., Graneto, M. J., Lee, L. F., Malecha, J. W., Miyashiro, J. M., et al. (1997) · Journal of Medicinal Chemistry · doi:10.1021/jm960803q · Cited by 1,965
Fluorine in Medicinal Chemistry
Böhm, H., Banner, D., Bendels, S., Kansy, M., Kuhn, B., Müller, K., Obst‐Sander, U., & Stahl, M. (2004) · ChemBioChem · doi:10.1002/cbic.200301023 · Cited by 1,572
Fluorine in medicinal chemistry: A review of anti-cancer agents
Isanbor, C., & O’Hagan, D. (2006) · Journal of Fluorine Chemistry · doi:10.1016/j.jfluchem.2006.01.011 · Cited by 1,120
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Fluorine in medicinal chemistry: Recent therapeutic applications of fluorinated small molecules
Kirk, K. L. (2006) · Journal of Fluorine Chemistry · doi:10.1016/j.jfluchem.2006.06.007 · Cited by 900
The fluoroquinolone antibacterials: past, present and future perspectives
Appelbaum, P. C., & Hunter, P. A. (2000) · International Journal of Antimicrobial Agents · doi:10.1016/s0924-8579(00)00192-8 · Cited by 629
Metabolism of Fluorine-Containing Drugs
Park, B. K., Kitteringham, N. R., & O'Neill, P. M. (2001) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.41.1.443 · Cited by 610
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Self-citationHow Strong Is the Cα−H···OC Hydrogen Bond?
Vargas, R., Garza, J., Dixon, D. A., & Hay, B. P. (2000) · Journal of the American Chemical Society · doi:10.1021/ja993600a · Cited by 415
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Cited by
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design
Meanwell, N. A. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01788 · Cited by 2,655
Carbon Trifluoromethylation Reactions of Hydrocarbon Derivatives and Heteroarenes
Alonso, C., Martínez de Marigorta, E., Rubiales, G., & Palacios, F. (2015) · Chemical Reviews · doi:10.1021/cr500368h · Cited by 1,073
Chemical Aspects of Human and Environmental Overload with Fluorine
Han, J., Kiss, L., Mei, H., Remete, A. M., Ponikvar-Svet, M., Sedgwick, D. M., Roman, R., Fustero, S., Moriwaki, H., & Soloshonok, V. A. (2021) · Chemical Reviews · doi:10.1021/acs.chemrev.0c01263 · Cited by 537
Ertl, P., Altmann, E., & McKenna, J. M. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00754 · Cited by 429
Reich, K., Teixeira, H. D., de Bruin-Weller, M., Bieber, T., Soong, W., Kabashima, K., Werfel, T., Zeng, J., Huang, X., Hu, X., et al. (2021) · The Lancet · doi:10.1016/s0140-6736(21)00589-4 · Cited by 402
Metadata
- Authors
- Shah, P., & Westwell, A. D.
- Venue
- Journal of Enzyme Inhibition and Medicinal Chemistry
- Publisher
- Informa UK Limited
- Published
- 2007-01
- Volume
- 22
- Issue
- 5
- Pages
- 527-540
- ISSN
- 1475-6366 (ISSN-L)
- 1475-6374
- OpenAlex
- W2140310496
- Cited by
- 799
- References
- 33
- FWCI
- 7.58
- Type
- journal article
- Language
- en
- Open access
- bronze
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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).
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