The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
Analysis of Past and Present Synthetic Methodologies on Medicinal Chemistry: Where Have All the New Reactions Gone?: Miniperspective
Open accessAbstract
An analysis of chemical reactions used in current medicinal chemistry (2014), three decades ago (1984), and in natural product total synthesis has been conducted. The analysis revealed that of the current most frequently used synthetic reactions, none were discovered within the past 20 years and only two in the 1980s and 1990s (Suzuki-Miyaura and Buchwald-Hartwig). This suggests an inherent high bar of impact for new synthetic reactions in drug discovery. The most frequently used reactions were amide bond formation, Suzuki-Miyaura coupling, and SNAr reactions, most likely due to commercial availability of reagents, high chemoselectivity, and a pressure on delivery. We show that these practices result in overpopulation of certain types of molecular shapes to the exclusion of others using simple PMI plots. We hope that these results will help catalyze improvements in integration of new synthetic methodologies as well as new library design.
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Cites
ChEMBL: a large-scale bioactivity database for drug discovery
Gaulton, A., Bellis, L. J., Bento, A. P., Chambers, J., Davies, M., Hersey, A., Light, Y., McGlinchey, S., Michalovich, D., Al-Lazikani, B., et al. (2012) · Nucleic Acids Research · doi:10.1093/nar/gkr777 · Cited by 4,382
Cited by
Schneider, G. (2018) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2017.232 · Cited by 910
Late-stage C–H functionalization offers new opportunities in drug discovery
Guillemard, L., Kaplaneris, N., Ackermann, L., & Johansson, M. J. (2021) · Nature Reviews Chemistry · doi:10.1038/s41570-021-00300-6 · Cited by 837
The importance of synthetic chemistry in the pharmaceutical industry
Campos, K. R., Coleman, P. J., Alvarez, J. C., Dreher, S. D., Garbaccio, R. M., Terrett, N. K., Tillyer, R. D., Truppo, M. D., & Parmee, E. R. (2019) · Science · doi:10.1126/science.aat0805 · Cited by 668
DNA-encoded chemistry: enabling the deeper sampling of chemical space
Goodnow, R. A., Dumelin, C. E., & Keefe, A. D. (2017) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.213 · Cited by 621
Douglas, J. J., Sevrin, M. J., & Stephenson, C. R. J. (2016) · Organic Process Research & Development · doi:10.1021/acs.oprd.6b00125 · Cited by 361
Metadata
- Authors
- Brown, D. G., & Boström, J.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2015-12-01
- Volume
- 59
- Issue
- 10
- Pages
- 4443-4458
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2247581895
- Cited by
- 1,964
- References
- 1
- FWCI
- 25.22
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- Brown, D. G., & Boström, J. (2016). Analysis of Past and Present Synthetic Methodologies on Medicinal Chemistry: Where Have All the New Reactions Gone?: Miniperspective. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.5b01409
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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.
